43 results on '"Draghici, C"'
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2. OPEN EDUCATIONAL RESOURCES FOR LEARNING WASTE MANAGEMENT IN RURAL COMMUNITIES.
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ROTARU, C. M. SALCA, DRAGHICI, C., and SCHWEGMANN, S.
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WASTE management , *EDUCATIONAL resources , *ENVIRONMENTAL protection , *ENVIRONMENTAL education , *PUBLIC administration - Abstract
Environmental protection is close related with environmental education. Environmental education is as necessary in the educational system as outside it. The present study, starting from the perception of the representatives of the local rural public administration and the citizens of the rural communities on environmental protection issues: (i) highlights the need for information and education in the field of environmental protection, especially with regard to environmental legislation and waste management; (ii) demonstrates the usefulness of environmental educational projects and the use of open educational resources, as resources that can be easily adapted to the real needs of education and information. [ABSTRACT FROM AUTHOR]
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- 2023
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3. Unplanned Fatherhood is Not Sperm Donation: The Unduly Moralistic Approach to Natural Fathers in European Convention Case Law
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Draghici, C.
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HQ ,JN ,HM ,RA - Abstract
This article criticises the Strasbourg Court’s reluctance to recognise the familial association between a natural father and a child with whom he had no opportunity to establish effective bonds, unless the child was the product of a committed relationship (by analogy with marriage) and planned conception, whilst downgrading family aspirations to a (less protected) privacy interest if the birth resulted from an extra-marital or fleeting relationship. The author also laments the Court’s readiness to accept superficial justifications for interferences with the father’s private or ‘potential’ family life (where it finds it engaged), such as the refusal to order genetic tests or contact. The Court allows the ‘child’s best interests’ façade to accommodate the mother’s choice of partner (especially in the case of children conceived in adultery) and remains oblivious to the modern plural fatherhood (whereby the husband continues his parental role qua stepfather, without obliterating the natural father’s family life with the child). It is further argued that, to end the gender-based double standard in the treatment of natural parents, the case law must de-couple the father’s family life with the child from the quality of the adults’ relationship and the circumstances surrounding conception (save for narrow exceptions) and acknowledge that currently pater certus est.
- Published
- 2022
4. Divorced from Human Rights? English Divorce Law under human-Rights Scrutiny
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Draghici, C., Miles, J., Monk, D., and Probert, R.
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KD ,HN - Published
- 2022
5. Assisted dying
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Draghici, C. and Loveland, I.
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KD ,HN ,K1 ,R1 - Abstract
This book explores current human rights controversies arising in UK law, in the light of the way such matters have been dealt with in Canada.
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- 2021
6. Fast-Tracking Low-Value Financial Claims in the Family Court
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Draghici, C. and Burton, F.
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HQ ,KD - Published
- 2020
7. Laser-assisted additive technologies for the execution of dental restorative prostheses
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Moraru, E, primary, Dontu, O, additional, Rizescu, C, additional, Spanu, A, additional, Ciobanu, R, additional, and Draghici, C, additional
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- 2020
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8. Research Pratices with Young Children: Epistemological and Political Issues
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Draghici, C. Carmen, primary and Garnier, Pascale, additional
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- 2020
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9. Killing Journalists is Not Media Regulation: Private Rights, Collective Wrongs and the Impact of Impunity
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Draghici, C. and Woods, L.
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JX ,K1 - Abstract
This article, somewhat against the trend in that growing body of scholarship in this area, argues that there is a role for a new international instrument targeting the harassment of and violence against journalists. It supports this position by a review of UN and regional human rights jurisprudence, with an emphasis on hitherto undiscussed weaknesses, as well as by an analysis of loopholes in international humanitarian law. It concludes with suggestions for a new instrument, providing better safeguards for both journalists and societal interests in the media, and highlights how such an instrument would tackle the problems in the existing framework.
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- 2019
10. Equal Marriage, Unequal Civil Partnership: A Bizarre Case of Discrimination in Europe
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Draghici, C.
- Abstract
The fact that heterosexual couples still cannot form civil partnerships after the introduction of gender-neutral marriage contravenes Articles 8 and 14 of the European Convention for the Protection of Human Rights and Fundamental Freedoms 1950. Albeit optional under the Convention (like adoption, parental leave or child benefits), civil partnership is an institution engaging the right to respect for family life and its domestic regulation demands conformity with Convention principles, including non-discrimination. This article contrasts states' wide margin of appreciation in matrimonial matters under Article 12 with the limited discretion under Article 8 and discusses the strict proportionality test applicable to differences in treatment exclusively based on sexual orientation. It dismisses the justifications espoused by executive and judicial authorities in recent litigation for the indefinite postponement of reform, namely the overestimated costs of legislative amendment, the subordination of the equality principle to the number of takers, and attempts to gauge social demand through post-2014 statistics on gay partnerships. Finally, it provides arguments for removing discrimination by opening civil partnership to opposite-sex couples rather than abolishing it: obviating hardship for family units lawfully constituted abroad, ensuring privacy for individuals whose disclosure of civil status reveals sexual orientation, and fostering a pluralist, tolerant society, accommodating ideological objections to marriage.
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- 2017
11. Massive open on-line courses in open educational resources and e-learning for toxicology courses
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GIROTTI, STEFANO, FERRARI, LUCA, PROTTI, MICHELE, MERCOLINI, LAURA, Draghici, C., Viorica Popescu, Simona Dobrinas, Girotti, S., Ferrari, L., Protti, M., Mercolini, L., and Draghici, C.
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Chemistry - Abstract
MASSIVE OPEN ON-LINE COURSES IN OPEN EDUCATIONAL RESOURCES AND E-LEARNING FOR TOXICOLOGY COURSES Stefano GIROTTI1, Luca FERRARI2, Michele PROTTI1, Laura MERCOLINI1, Camelia DRAGHICI3 1Department of Pharmacy and Biotechnology FaBiT, Via San Donato 15, Alma Mater Studiorum - Università di Bologna, Bologna,40127, Italy 2Dipartimento di Scienze dell' Educazione 'G.M. Bertin', Alma Mater Studiorum - Università di Bologna, Via Filippo Re 6, 40126 Bologna, Italy 3Department of Product Design, Mechatronics and Environment, Transilvania University of Brasov, 29 Eroilor Blv, 500036 Brasov, Romania Remarkably, owing to the lack of European Massive Open On-line Courses (MOOCs) [1] in the field of the Toxicology and major differences in the teaching and learning of this important subject at various European biologically oriented faculties, we will present our TOX-OER European project which develops a scientific and pedagogical joint between research in the field of toxicology and MOOC pedagogical design [2]. This will consist in a guideline to support partners during: a) the creation of accessible Open Educational Resources (OER); b) course & module management; c) the implementation, monitoring and evaluation of individual and social learning activities. This procedure will contribute to the promotion of using the learning outcomes in the design and delivery of educational programs and activities in favor of pupils, students, young people, trainees, adult learners. Furthermore, the TOX-OER project could create the conditions for the RECOGNITION and CERTIFICATION (ECTS credits) of learning achievements, at least between partners. Finally, throughout the duration of the project, the partners involved in the educational tasks will manage a virtual space (server) within which the MOOC platform will be installed, and where all the Open Educational Resources will be available. TOX-OER project is coordinated by Universidad de Salamanca and partners are: Università di Bologna, Italy; Transilvania University of Brasov, Romania; Univerzita Karlova V Praze, Czech Republic; Universidade do Porto, Portugal; Space Research and Technology Institute, Bulgaria; Kymenlaakson Ammattikorkeakoululu Oy, Finland. [1] Chiappe, A., & Arias, V. (2015). Understanding reusability as a key factor for open education: A review. The International Review of Research in Open and Distributed Learning, 16(1). Retrieved from http://www.irrodl.org/index.php/irrodl/article/view/2042 ISSN: 1492-3831 [2] https://www.youtube.com/watch?v=U9lHtNLHP4Y
- Published
- 2016
12. ECHR: Right to marry
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Draghici, C.
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KD - Abstract
The right to marry is guaranteed under the European Convention on Human Rights ECHR)in art.12, which reads: "Men and women of marriageable age have the right to marry and to found a family, according to the national laws governing the exercise of this right". This provision was given effect in the UK through the enactment of the Human Rights Act 1998, which incorporated ECHR rights, allowing domestic litigants to rely on them before the British courts. The express referral to "national laws" in art.12 indicates that States may legitimately impose restrictions on the exercise of this right, such as bars on marriage between persons who fall within the prohibited degrees of a relationship, a minimum marriageable age, and the requirement to comply with certain formalities for the valid celebration of marriages. The Convention institutions maintain, nevertheless, the power to scrutinise any such restrictions, and ensure that domestic law strikes a fair balance between the prevention of objectionable marriages and the protection of individual rights against social prejudice. Controversial issues in this area include same-sex marriage, polygamous, underage and religious marriage within ethnic minority communities, transsexuals' right to marry according to the newly acquired gender, the suspension of the exercise of the right in circumstances involving deprivation of liberty, the right to re-marry, and the right to divorce and re-acquire the capacity to marry.
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- 2015
13. The Blanket Ban on Assisted Suicide: Between Moral Paternalism and Utilitarian Justice
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Draghici, C.
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K1 - Abstract
The article analyses the ramifications of the Supreme Court’s 2014 Nicklinson judgment. It argues that the majority approach to a declaration of incompatibility as judicial incursion into legislative territory does not rest convincingly on the distribution of power envisaged by the Human Rights Act. Contrasting the domestic courts’ wider prerogatives to develop human rights with the self-restraint of the Strasbourg Court, driven by the margin of appreciation, the author contends that the judgment fails to protect the right to personal autonomy. Unlike the Strasbourg Court, reserved in matters pertaining to the sensitive field of bioethics, where no European consensus can legitimise progressive judgments, domestic courts have more leeway to signal to the legislature that the manner in which discretion was exercised does not strike a fair balance between competing interests. A development in this direction would find support in the general Strasbourg approach to blanket bans in other controversial areas.
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- 2015
14. MASSIVE OPEN ONLINE COURSES (MOOCS) WITH OPEN EDUCATIONAL RESOURCES FOR TOXICOLOGY LEARNING - DRUGS AND POLLUTANTS AS XENOBIOTICS
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Stefano Girotti, Ileana Manciulea, Michele Protti, Lucia Dumitrescu, Laura Mercolini, Camelia Draghici, Anca Vasilescu, Dana Perniu, Luca Ferrari, Manciulea, I., Vasilescu, A., Girotti, S., Ferrari, L., Protti, M., Mercolini, L., Dumitrescu, L., and Perniu, D., Draghici, C.
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Czech ,Environmental Engineering ,Subject (documents) ,Management, Monitoring, Policy and Law ,Pollution ,Open educational resources ,language.human_language ,Internationalization of Higher Education ,Toxicology ,drugs, massive open online courses, open educational resources, pollutants, toxicology ,Political science ,General partnership ,language ,Erasmus+ - Abstract
Due to the lack of European Massive Open Online Courses (MOOCs) in the field of the Toxicology and the major differences in the styles of teaching and learning of this important subject in amongst various European life science-oriented institutions, the European Erasmus+ project “Learning Toxicology through Open Educational Resources (TOX-OER)” was developed and implemented. Considering the complexity and heterogeneity of the toxicology field, the TOX-OER project main objective was to develop and share toxicology-related knowledge and skills among students/ earners from seven countries, which promote the internationalization of Higher Education Institutions in Europe but also in countries from other continents. The project was coordinated by Universidad de Salamanca (Spain), and the partners were: Space Research and Technology Institute (Bulgaria), Univerzita Karlova V Praze (Czech Republic), South-Eastern Finland University of Applied Sciences (Finland), Università di Bologna (Italy), Universidade do Porto (Portugal) and Universitatea Transilvania din Brasov (Romania). One of the goals/ objectives of the project is the dissemination, popularizing the information and reaching potentially interested people who can benefit from the offered courses. The aim of this paper is to present and analyze part of the TOX-OER’s outcomes developed by the project’s partnership, especially the modules/ topics related to the drugs, gaseous and persistent organic pollutants, as the principal groups of xenobiotics.
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- 2019
15. Experiments and Calculation on New N,N- bis -Tetrahydroacridines.
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Hrubaru MM, Draghici C, Ngounoue Kamga FA, Diacu E, Egemonye TC, Ekennia AC, and Ungureanu EM
- Abstract
Tetrahydroacridines arouse particular interest due to the potential possibilities of application in the medical field and protection against corrosion. Bis -tetrahydroacridines were newly synthesized by Pfitzinger condensation of 5,5'-(ethane-1,2-diyl) diindoline-2,3-dione with several cyclanones. NMR, MS, and FT-IR were used to prove their molecular structure. In addition, a computer-aided study was performed for the lowest energy conformers of each structure, in vacuum conditions, at ground state using DFT models to assess their electronic properties. UV-Vis and voltammetric methods (cyclic voltammetry, differential pulse voltammetry, and rotating disk electrode voltammetry) were used to investigate their optical and electrochemical properties. The results obtained for these π-conjugated heteroaromatic compounds lead to the conclusion that they have real potential in applications in different fields such as pharmaceuticals and especially as corrosion inhibitors.
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- 2024
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16. Current Perspectives on Biological Screening of Newly Synthetised Sulfanilamide Schiff Bases as Promising Antibacterial and Antibiofilm Agents.
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Coanda M, Limban C, Draghici C, Ciobanu AM, Grigore GA, Popa M, Stan M, Larion C, Avram S, Mares C, Ciornei MC, Dabu A, Hudita A, Galateanu B, Pintilie L, and Nuta DC
- Abstract
Growing resistance to antimicrobials, combined with pathogens that form biofilms, presents significant challenges in healthcare. Modifying current antimicrobial agents is an economical approach to developing novel molecules that could exhibit biological activity. Thus, five sulfanilamide Schiff bases were synthesized under microwave irradiation and characterized spectroscopically and in silico. They were evaluated for their antimicrobial and antibiofilm activities against both Gram-positive and Gram-negative bacterial strains. Their cytotoxic potential against two cancer cell lines was also determined. Gram-positive bacteria were susceptible to the action of these compounds. Derivatives 1b and 1d inhibited S. aureus 's growth (MIC from 0.014 mg/mL) and biofilm (IC from 0.029 mg/mL), while compound 1e was active against E. faecalis' s planktonic and sessile forms. Two compounds significantly reduced cell viability at 5 μg/mL after 24 h of exposure ( 1d -HT-29 colorectal adenocarcinoma cells, 1c -LN229 glioblastoma cells). A docking study revealed the increased binding affinities of these derivatives compared to sulfanilamide. Hence, these Schiff bases exhibited higher activity compared to their parent drug, with halogen groups playing a crucial role in both their antimicrobial and cytotoxic effects.
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- 2024
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17. Synthesis of 1,3,4-Thiadiazole Derivatives and Their Anticancer Evaluation.
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Stecoza CE, Nitulescu GM, Draghici C, Caproiu MT, Hanganu A, Olaru OT, Mihai DP, Bostan M, and Mihaila M
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- Molecular Structure, Structure-Activity Relationship, Cell Proliferation, Drug Screening Assays, Antitumor, Cell Line, Tumor, Antineoplastic Agents chemistry, Thiadiazoles chemistry
- Abstract
Thiadiazole derivatives have garnered significant attention in the field of medicinal chemistry due to their diverse pharmacological activities, including anticancer properties. This article presents the synthesis of a series of thiadiazole derivatives and investigates their chemical characterization and potential anticancer effects on various cell lines. The results of the nuclear magnetic resonance (NMR) analyses confirmed the successful formation of the target compounds. The anticancer potential was evaluated through in silico and in vitro cell-based assays using LoVo and MCF-7 cancer lines. The assays included cell viability, proliferation, apoptosis, and cell cycle analysis to assess the compounds' effects on cancer cell growth and survival. Daphnia magna was used as an invertebrate model for the toxicity evaluation of the compounds. The results revealed promising anticancer activity for several of the synthesized derivatives, suggesting their potential as lead compounds for further drug development. The novel compound 2g , 5-[2-(benzenesulfonylmethyl)phenyl]-1,3,4-thiadiazol-2-amine, demonstrated good anti-proliferative effects, exhibiting an IC
50 value of 2.44 µM against LoVo and 23.29 µM against MCF-7 after a 48-h incubation and little toxic effects in the Daphnia test.- Published
- 2023
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18. Novel Strigolactone Mimics That Modulate Photosynthesis and Biomass Accumulation in Chlorella sorokiniana .
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Popa DG, Georgescu F, Dumitrascu F, Shova S, Constantinescu-Aruxandei D, Draghici C, Vladulescu L, and Oancea F
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- Biomass, Photosynthesis, Furans pharmacology, Furans metabolism, Chlorella metabolism, Microalgae metabolism
- Abstract
In terrestrial plants, strigolactones act as multifunctional endo- and exo-signals. On microalgae, the strigolactones determine akin effects: induce symbiosis formation with fungi and bacteria and enhance photosynthesis efficiency and accumulation of biomass. This work aims to synthesize and identify strigolactone mimics that promote photosynthesis and biomass accumulation in microalgae with biotechnological potential. Novel strigolactone mimics easily accessible in significant amounts were prepared and fully characterized. The first two novel compounds contain 3,5-disubstituted aryloxy moieties connected to the bioactive furan-2-one ring. In the second group of compounds, a benzothiazole ring is connected directly through the cyclic nitrogen atom to the bioactive furan-2-one ring. The novel strigolactone mimics were tested on Chlorella sorokiniana NIVA-CHL 176. All tested strigolactones increased the accumulation of chlorophyll b in microalgae biomass. The SL-F3 mimic, 3-(4-methyl-5-oxo-2,5-dihydrofuran-2-yl)-3 H -benzothiazol-2-one ( 7 ), proved the most efficient. This compound, applied at a concentration of 10
-7 M, determined a significant biomass accumulation, higher by more than 15% compared to untreated control, and improved the quantum yield efficiency of photosystem II. SL-F2 mimic, 5-(3,5-dibromophenoxy)-3-methyl-5 H -furan-2-one ( 4 ), applied at a concentration of 10-9 M, improved protein production and slightly stimulated biomass accumulation. Potential utilization of the new strigolactone mimics as microalgae biostimulants is discussed., Competing Interests: The authors declare no conflict of interest.- Published
- 2023
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19. Pancreaticogastrostomy versus Pancreaticojejunostomy and the Proposal of a New Postoperative Pancreatic Fistula Risk Score.
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Mastalier B, Cauni V, Tihon C, Septimiu Petrutescu M, Ghita B, Popescu V, Andras D, Radu IM, Vlasceanu VG, Floroiu MF, Draghici C, Botezatu C, Cretoiu D, Varlas VN, and Lazar AM
- Abstract
Despite the substantial decrease in mortality rates following a pancreaticoduodenectomy to less than 5%, morbidity rates remain significant, reaching even 73%. Postoperative pancreatic fistula is one of the most frequent major complications and is significantly associated with other complications, including patient death. Currently, there is no consensus regarding the ideal type of pancreatic anastomosis, as the question of the choice between a pancreaticogastrostomy and pancreaticojejunostomy is still open. Furthermore, worldwide implementation of an ideal pancreatic fistula risk prediction score is missing. Our study found several significant predictive factors for the postoperative occurrence of fistulas, such as the soft consistency of the pancreas, non-dilated Wirsung duct, important intraoperative blood loss, other perioperative complications, preoperative patient hypoalbuminemia, and patient weight loss. Our study also revealed that for patients who exhibit fistula risk factors, pancreaticogastrostomy demonstrates a significantly lower pancreatic fistula rate than pancreaticojejunostomy. The occurrence of pancreatic fistulas has been significantly associated with the development of other postoperative major complications, and patient death. As the current pancreatic fistula risk scores proposed by various authors have not been consensually validated, we propose a simple, easy-to-use, and sensitive score for the risk prediction of postoperative pancreatic fistula occurrence based on important predictors from statistical analyses that have also been found to be significant by most of the reported studies. The new pancreatic fistula risk score proposed by us could be extremely useful for improved therapeutic management of cephalic pancreaticoduodenectomy patients.
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- 2023
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20. Synthesis, Characterization and Cytotoxic Evaluation of New Pyrrolo[1,2- b ]pyridazines Obtained via Mesoionic Oxazolo-Pyridazinones.
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Ivan BC, Barbuceanu SF, Hotnog CM, Olaru OT, Anghel AI, Ancuceanu RV, Mihaila MA, Brasoveanu LI, Shova S, Draghici C, Nitulescu GM, and Dumitrascu F
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- Animals, Humans, Molecular Structure, Structure-Activity Relationship, Drug Screening Assays, Antitumor, Cell Proliferation, Pyridazines chemistry, Antineoplastic Agents chemistry
- Abstract
New pyrrolo[1,2- b ]pyridazines were synthesized by 3 + 2 cycloaddition reaction between mesoionic oxazolo-pyridazinones and methyl/ethyl propiolate. The mesoionic compounds were generated in situ by action of acetic anhydride on 3(2 H )pyridazinone acids obtained from corresponding esters by alkaline hydrolysis followed by acidification. The structures of the compounds were confirmed by elemental analyses and IR,
1 H-NMR,13 C-NMR, and X-ray diffraction data. The regioselectivity of cycloaddition was evidenced by NMR spectroscopy and confirmed by X-ray analysis. The compounds were evaluated for their cytotoxicity on plant cells ( Triticum aestivum L.) and crustacean animal cells ( Artemia franciscana Kellogg and Daphnia magna Straus). The results indicated that the tested compounds exhibited low toxicity on the plant cell (IC50 values higher than 200 µM), while on Artemia nauplii no lethality was observed. Daphnia magna assay showed that pyrrolo[1,2- b ]pyridazines 5a and 5c could exhibit toxic effects, whereas, for the other compounds, toxicity was low to moderate. Also, the cytotoxic effects of the compounds were tested on three human adenocarcinoma-derived adherent cell lines (colon LoVo, ovary SK-OV-3, breast MCF-7). The in vitro compound-mediated cytotoxicity assays, performed by the MTS technique, demonstrated dose- and time-dependent cytotoxic activity for several compounds, the highest anti-tumor activity being observed for 5a , 2c, and 5f , especially against colon cancer cells.- Published
- 2023
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21. Ni(II)-Salophen-Comprehensive Analysis on Electrochemical and Spectral Characterization and Biological Studies.
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Ngounoue Kamga FA, Hrubaru MM, Enache O, Diacu E, Draghici C, Tecuceanu V, Ungureanu EM, Nkemone S, and Ndifon PT
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- Antifungal Agents pharmacology, Antifungal Agents chemistry, Spectroscopy, Fourier Transform Infrared, Ligands, Microbial Sensitivity Tests, Schiff Bases chemistry, Anti-Infective Agents pharmacology, Anti-Infective Agents chemistry, Coordination Complexes pharmacology, Coordination Complexes chemistry
- Abstract
New aspects of the Ni(II)-salophen complex and salophen ligand precursor were found during deep electrochemical and optical characterization, as well as biological studies for new pharmacological applications. Physicochemical and spectroscopic methods (
1 H- and13 C-NMR, FT-IR and UV-Vis, electrospray ionization mass spectroscopy, thermogravimetric analysis, and molar conductance measurements) were also used to prove that the salophen ligand acts as a tetradentate and coordinates to the central metal through nitrogen and oxygen atoms. The electrochemical behavior of the free Schiff salophen ligand (H2 L ) and its Ni(II) complex (Ni(II) L ) was deeply studied in tetrabutylammonium perchlorate solutions in acetonitrile via CV, DPV, and RDE. Blue films on the surfaces of the electrodes as a result of the electropolymerization processes were put in evidence and characterized via CV and DPV. (H2 L ) and Ni(II) L complexes were tested for their antimicrobial, antifungal, and antioxidant activity, showing good antimicrobial and antifungal activity against several bacteria and fungi.- Published
- 2023
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22. New Heterocyclic Compounds from Oxazol-5(4 H )-one and 1,2,4-Triazin-6(5 H )-one Classes: Synthesis, Characterization and Toxicity Evaluation.
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Barbuceanu SF, Rosca EV, Apostol TV, Socea LI, Draghici C, Farcasanu IC, Ruta LL, Nitulescu GM, Iscrulescu L, Pahontu EM, Boscencu R, Saramet G, and Olaru OT
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- Sodium Acetate, Spectroscopy, Fourier Transform Infrared, Saccharomyces cerevisiae, Oxazolone chemistry, Triazines toxicity
- Abstract
This paper describes the synthesis of new heterocycles from oxazol-5(4 H )-one and 1,2,4-triazin-6(5 H )-one classes containing a phenyl-/4-bromophenylsulfonylphenyl moiety. The oxazol-5(4 H )-ones were obtained via condensation of 2-(4-(4-X-phenylsulfonyl)benzamido)acetic acids with benzaldehyde/4-fluorobenzaldehyde in acetic anhydride and in the presence of sodium acetate. The reaction of oxazolones with phenylhydrazine, in acetic acid and sodium acetate, yielded the corresponding 1,2,4-triazin-6(5 H )-ones. The structures of the compounds were confirmed using spectral (FT-IR,
1 H-NMR,13 C-NMR, MS) and elemental analysis. The toxicity of the compounds was evaluated on Daphnia magna Straus crustaceans and on the budding yeast Saccharomyces cerevisiae . The results indicate that both the heterocyclic nucleus and halogen atoms significantly influenced the toxicity against D. magna , with the oxazolones being less toxic than triazinones. The halogen-free oxazolone had the lowest toxicity, and the fluorine-containing triazinone exhibited the highest toxicity. The compounds showed low toxicity against yeast cells, apparently due to the activity of plasma membrane multidrug transporters Pdr5 and Snq2. The predictive analyses indicated an antiproliferative effect as the most probable biological action. The PASS prediction and CHEMBL similarity studies show evidence that the compounds could inhibit certain relevant oncological protein kinases. These results correlated with toxicity assays suggest that halogen-free oxazolone could be a good candidate for future anticancer investigations.- Published
- 2023
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23. New Pyrazolo-Benzimidazole Mannich Bases with Antimicrobial and Antibiofilm Activities.
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Zalaru C, Dumitrascu F, Draghici C, Tarcomnicu I, Marinescu M, Nitulescu GM, Tatia R, Moldovan L, Popa M, and Chifiriuc MC
- Abstract
A new series of pyrazolo-benzimidazole hybrid Mannich bases were synthesized, characterized by
1 H-NMR,13 C-NMR, IR, UV-Vis, MS, and elemental analysis. In vitro cytotoxicity of the new compounds studied on fibroblast cells showed that the newly synthesized pyrazolo-benzimidazole hybrid derivatives were noncytotoxic until the concentration of 1 μM and two compounds presented a high degree of biocompatibility. The antibacterial and antibiofilm activity of the newly synthesized compounds was assayed on Gram-positive Staphylococcus aureus ATCC25923, Enterococcus faecalis ATCC29212, and Gram-negative Pseudomonas aeruginosa ATCC27853, Escherichia coli ATCC25922 strains. All synthesized compounds 5a-g are more active against all three tested bacterial strains Staphylococcus aureus ATCC25923, Enterococcus faecalis ATCC29212, and Escherichia coli ATCC25922 than reference drugs (Metronidazole, Nitrofurantoin), with the exception of compounds 5d and 5g , which are less active compared to Nitrofurantoin, and all synthesized compounds 5a-g are more active against Pseudomonas aeruginosa ATCC27853 compared to reference drugs (Metronidazole, Nitrofurantoin). Compound 5f showed the best activity against Staphylococcus aureus ATCC 25923, with a MIC of 150 μg/mL and has also inhibited the biofilm formed by all the bacterial strains, having an MBIC of 310 µg/mL compared to the reference drugs (Metronidazole, Nitrofurantoin).- Published
- 2022
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24. New Pyrrole Derivatives as Promising Biological Agents: Design, Synthesis, Characterization, In Silico, and Cytotoxicity Evaluation.
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Ivan BC, Barbuceanu SF, Hotnog CM, Anghel AI, Ancuceanu RV, Mihaila MA, Brasoveanu LI, Shova S, Draghici C, Olaru OT, Nitulescu GM, Dinu M, and Dumitrascu F
- Subjects
- Animals, Biological Factors pharmacology, Cell Line, Tumor, Cell Proliferation, Drug Screening Assays, Antitumor, Endothelial Cells, Female, Humans, Molecular Structure, Structure-Activity Relationship, Antineoplastic Agents chemistry, Pyrroles chemistry
- Abstract
The current study describes the synthesis, physicochemical characterization and cytotoxicity evaluation of a new series of pyrrole derivatives in order to identify new bioactive molecules. The new pyrroles were obtained by reaction of benzimidazolium bromide derivatives with asymmetrical acetylenes in 1,2-epoxybutane under reflux through the Huisgen [3 + 2] cycloaddition of several ylide intermediates to the corresponding dipolarophiles. The intermediates salts were obtained from corresponding benzimidazole with bromoacetonitrile. The structures of the newly synthesized compounds were confirmed by elemental analysis, spectral techniques (i.e., IR,
1 H-NMR and13 C-NMR) and single-crystal X-ray analysis. The cytotoxicity of the synthesized compounds was evaluated on plant cells (i.e., Triticum aestivum L.) and animal cells using aquatic crustaceans (i.e., Artemia franciscana Kellogg and Daphnia magna Straus). The potential antitumor activity of several of the pyrrole derivatives was studied by performing in vitro cytotoxicity assays on human adenocarcinoma-derived cell lines (i.e., LoVo (colon), MCF-7 (breast), and SK-OV-3 (ovary)) and normal human umbilical vein endothelial cells (HUVECs). The obtained results of the cytotoxicity assessment indicated that the tested compounds had nontoxic activity on Triticum aestivum L., while on Artemia franciscana Kellogg nauplii, only compounds 2c and 4c had moderate toxicity. On Daphnia magna , 4b and 4c showed high toxicity; 2a , 2b , and 2c moderate to high toxicity; only 4a and 4d were nontoxic. The compound-mediated cytotoxicity assays showed that several pyrrole compounds demonstrated dose- and time-dependent cytotoxic activity against all tested tumor cell lines, the highest antitumor properties being achieved by 4a and its homologue 4d , especially against LoVo colon cells.- Published
- 2022
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25. Synthesis and Toxicity Evaluation of New Pyrroles Obtained by the Reaction of Activated Alkynes with 1-Methyl-3-(cyanomethyl)benzimidazolium Bromide.
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Ivan BC, Dumitrascu F, Anghel AI, Ancuceanu RV, Shova S, Dumitrescu D, Draghici C, Olaru OT, Nitulescu GM, Dinu M, and Barbuceanu SF
- Subjects
- Chemistry Techniques, Synthetic, Models, Molecular, Molecular Structure, Pyrroles chemistry, Spectrum Analysis, Toxicity Tests, Toxicology methods, Alkynes chemistry, Benzimidazoles chemistry, Bromides chemistry, Pyrroles chemical synthesis, Pyrroles toxicity
- Abstract
A series of new pyrrole derivatives were designed as chemical analogs of the 1,4-dihydropyridines drugs in order to develop future new calcium channel blockers. The new tri- and tetra-substituted N -arylpyrroles were synthesized by the one-pot reaction of 1-methyl-3-cyanomethyl benzimidazolium bromide with substituted alkynes having at least one electron-withdrawing substituent, in 1,2-epoxybutane, acting both as the solvent and reagent to generate the corresponding benzimidazolium N3-ylide. The structural characterization of the new substituted pyrroles was based on IR, NMR spectroscopy as well as on single crystal X-ray analysis. The toxicity of the new compounds was assessed on the plant cell using Triticum aestivum L. species and on the animal cell using Artemia franciscana Kellogg and Daphnia magna Straus crustaceans. The compounds showed minimal phytotoxicity on Triticum rootlets and virtually no acute toxicity on Artemia nauplii, while on Daphnia magna , it induced moderate to high toxicity, similar to nifedipine. Our research indicates that the newly synthetized pyrrole derivatives are promising molecules with biological activity and low acute toxicity.
- Published
- 2021
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26. Synthesis, In Silico and In Vitro Evaluation of Antimicrobial and Toxicity Features of New 4-[(4-Chlorophenyl)sulfonyl]benzoic Acid Derivatives.
- Author
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Apostol TV, Chifiriuc MC, Draghici C, Socea LI, Marutescu LG, Olaru OT, Nitulescu GM, Pahontu EM, Saramet G, and Barbuceanu SF
- Subjects
- Animals, Anti-Infective Agents chemistry, Anti-Infective Agents pharmacology, Benzoic Acid chemistry, Benzoic Acid pharmacology, Biofilms drug effects, Daphnia drug effects, Drug Evaluation, Preclinical, Microbial Sensitivity Tests, Proton Magnetic Resonance Spectroscopy, Toxicity Tests, Anti-Infective Agents chemical synthesis, Anti-Infective Agents toxicity, Benzoic Acid chemical synthesis, Benzoic Acid toxicity, Computer Simulation
- Abstract
The multi-step synthesis, physico-chemical characterization, and biological activity of novel valine-derived compounds, i.e., N -acyl-α-amino acids, 1,3-oxazol-5(4 H )-ones, N -acyl-α-amino ketones, and 1,3-oxazoles derivatives, bearing a 4-[(4-chlorophenyl)sulfonyl]phenyl moiety are reported here. The structures of the newly synthesized compounds were confirmed by spectral (UV-Vis, FT-IR, MS,
1 H- and13 C-NMR) data and elemental analysis results, and their purity was determined by RP-HPLC. The new compounds were assessed for their antimicrobial activity and toxicity to aquatic crustacean Daphnia magna . Also, in silico studies regarding their potential mechanism of action and toxicity were performed. The antimicrobial evaluation revealed that the 2-{4-[(4-chlorophenyl)sulfonyl]benzamido}-3-methylbutanoic acid and the corresponding 1,3-oxazol-5(4 H )-one exhibited antimicrobial activity against Gram-positive bacterial strains and the new 1,3-oxazole containing a phenyl group at 5-position against the C. albicans strain.- Published
- 2021
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27. Synthesis and Biological Evaluation of New N -Acyl-α-amino Ketones and 1,3-Oxazoles Derivatives.
- Author
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Apostol TV, Marutescu LG, Draghici C, Socea LI, Olaru OT, Nitulescu GM, Pahontu EM, Saramet G, Enache-Preoteasa C, and Barbuceanu SF
- Subjects
- Biofilms drug effects, Molecular Structure, Structure-Activity Relationship, Spectroscopy, Fourier Transform Infrared, Oxazoles chemistry, Oxazoles pharmacology, Oxazoles chemical synthesis, Ketones chemistry, Ketones pharmacology, Ketones chemical synthesis, Microbial Sensitivity Tests, Anti-Bacterial Agents pharmacology, Anti-Bacterial Agents chemical synthesis, Anti-Bacterial Agents chemistry
- Abstract
In order to develop novel bioactive substances with potent activities, some new valine-derived compounds incorporating a 4-(phenylsulfonyl)phenyl fragment, namely, acyclic precursors from N -acyl-α-amino acids and N -acyl-α-amino ketones classes, and heterocycles from the large family of 1,3-oxazole-based compounds, were synthesized. The structures of the new compounds were established using elemental analysis and spectral (UV-Vis, FT-IR, MS, NMR) data, and their purity was checked by reversed-phase HPLC. The newly synthesized compounds were evaluated for their antimicrobial and antibiofilm activities, for toxicity on D. magna , and by in silico studies regarding their potential mechanism of action and toxicity. The 2-aza-3-isopropyl-1-[4-(phenylsulfonyl)phenyl]-1,4-butanedione 4b bearing a p -tolyl group in 4-position exhibited the best antibacterial activity against the planktonic growth of both Gram-positive and Gram-negative strains, while the N -acyl-α-amino acid 2 and 1,3-oxazol-5(4 H )-one 3 inhibited the Enterococcus faecium biofilms. Despite not all newly synthesized compounds showing significant biological activity, the general scaffold allows several future optimizations for obtaining better novel antimicrobial agents by the introduction of various substituents on the phenyl moiety at position 5 of the 1,3-oxazole nucleus.
- Published
- 2021
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28. Synthesis of 1-(2-Fluorophenyl)pyrazoles by 1,3-Dipolar Cycloaddition of the Corresponding Sydnones.
- Author
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Dumitrescu D, Shova S, Draghici C, Popa MM, and Dumitrascu F
- Abstract
3-Arylsydnones bearing fluorine and bromine atoms on the benzene ring were synthesized from N -nitroso-2-fluorophenylglycines and characterized by NMR spectroscopy. These were employed further in synthesis of the corresponding 1-(2-fluorophenyl)pyrazoles by 1,3-dipolar cycloaddition reaction with dimethyl acetylenedicarboxylate (DMAD) as activated dipolarophile. The sydnones as reaction intermediates were characterized by single crystal X-ray diffraction analysis showing interesting features such as halogen bonding as an important interaction in modeling the crystal structure.
- Published
- 2021
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29. Neuroendocrine Factors in Melanoma Pathogenesis.
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Scheau C, Draghici C, Ilie MA, Lupu M, Solomon I, Tampa M, Georgescu SR, Caruntu A, Constantin C, Neagu M, and Caruntu C
- Abstract
Melanoma is one of the most aggressive skin cancers with a sharp rise in incidence in the last decades, especially in young people. Recognized as a significant public health issue, melanoma is studied with increasing interest as new discoveries in molecular signaling and receptor modulation unlock innovative treatment options. Stress exposure is recognized as an important component in the immune-inflammatory interplay that can alter the progression of melanoma by regulating the release of neuroendocrine factors. Various neurotransmitters, such as catecholamines, glutamate, serotonin, or cannabinoids have also been assessed in experimental studies for their involvement in the biology of melanoma. Alpha-MSH and other neurohormones, as well as neuropeptides including substance P, CGRP, enkephalin, beta-endorphin, and even cellular and molecular agents (mast cells and nitric oxide, respectively), have all been implicated as potential factors in the development, growth, invasion, and dissemination of melanoma in a variety of in vitro and in vivo studies. In this review, we provide an overview of current evidence regarding the intricate effects of neuroendocrine factors in melanoma, including data reported in recent clinical trials, exploring the mechanisms involved, signaling pathways, and the recorded range of effects.
- Published
- 2021
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30. Synthesis and Anticancer Evaluation of New 1,3,4-Oxadiazole Derivatives.
- Author
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Stecoza CE, Nitulescu GM, Draghici C, Caproiu MT, Olaru OT, Bostan M, and Mihaila M
- Abstract
In order to develop novel chemotherapeutic agents with potent anticancer activities, a series of new 2,5-diaryl/heteroaryl-1,3,4-oxadiazoles were designed and synthesized. The structures of the new compounds were established using elemental analyses, IR and NMR spectral data. The compounds were evaluated for their anticancer potential on two standardized human cell lines, HT-29 (colon adenocarcinoma) and MDA-MB-231 (breast adenocarcinoma). Cytotoxicity was measured by MTS assay, while cell cycle arrest and apoptosis assays were conducted using a flow cytometer, the results showing that the cell line MDA-MB-231 is more sensitive to the compounds' action. The results of the predictive studies using the PASS application and the structural similarity analysis indicated STAT3 and miR-21 as the most probable pharmacological targets for the new compounds. The promising effect of compound 3e , 2-[2-(phenylsulfanylmethyl)phenyl]-5-(4-pyridyl)-1,3,4-oxadiazole, especially on the MDA-MB-231 cell line motivates future studies to improve the anticancer profile and to reduce the toxicological risks. It is worth noting that 3e produced a low toxic effect in the D. magna 24 h assay and the predictive studies on rat acute toxicity suggest a low degree of toxic risks.
- Published
- 2021
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31. Introducing chirality in halogenated 3-arylsydnones and their corresponding 1-arylpyrazoles obtained by 1,3-dipolar cycloaddition.
- Author
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Popa MM, Shova S, Hrubaru M, Barbu L, Draghici C, Dumitrascu F, and Dumitrescu DE
- Abstract
New 1-arylpyrazoles substituted with halogen atoms (Br, I) were synthesized from the corresponding sydnones by 1,3-dipolar cycloaddition. By introduction of a prochiral group such as isopropyl, in the ortho position of the benzene ring, in the starting phenylglycine 1 the rotamers caused by the hindered rotation between the phenyl and the heterocyclic ring were detected by NMR spectroscopy for 1-arylpyrazoles and for the first time for 3-arylsydnones. The N -nitrosophenylglycines present E - Z stereoisomerism due to the partial C-N double bond character. All the new compounds were structurally characterized by NMR spectroscopy and confirmed by X-ray crystallography. The crystal structures of N -nitrosophenylglycine 2c and of the sydnone 3c present similar Br⋯Br type II halogen contacts., Competing Interests: There are no conflicts to declare., (This journal is © The Royal Society of Chemistry.)
- Published
- 2020
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32. In Silico and In Vitro Experimental Studies of New Dibenz[ b , e ]oxepin-11(6 H )one O-(arylcarbamoyl)-oximes Designed as Potential Antimicrobial Agents.
- Author
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Vlad IM, Nuta DC, Chirita C, Caproiu MT, Draghici C, Dumitrascu F, Bleotu C, Avram S, Udrea AM, Missir AV, Marutescu LG, and Limban C
- Subjects
- Biofilms growth & development, Cell Line, Humans, Anti-Infective Agents chemistry, Anti-Infective Agents pharmacology, Bacteria growth & development, Bacterial Physiological Phenomena drug effects, Biofilms drug effects, Candida albicans physiology, Computer Simulation, Oximes chemistry, Oximes pharmacology
- Abstract
In a drug-repurposing-driven approach for speeding up the development of novel antimicrobial agents, this paper presents for the first time in the scientific literature the synthesis, physico-chemical characterization, in silico analysis, antimicrobial activity against bacterial and fungal strains in planktonic and biofilm growth state, as well as the in vitro cytotoxicity of some new 6,11-dihydrodibenz[ b , e ]oxepin-11(6 H )one O-(arylcarbamoyl)oximes. The structures of intermediary and final substances (compounds 7a - j ) were confirmed by
1 H-NMR,13 C-NMR and IR spectra, as well as by elemental analysis. The in silico bioinformatic and cheminformatic studies evidenced an optimal pharmacokinetic profile for the synthesized compounds 7a - j , characterized by an average lipophilic character predicting good cell membrane permeability and intestinal absorption; low maximum tolerated dose for humans; potassium channels encoded by the hERG I and II genes as potential targets and no carcinogenic effects. The obtained compounds exhibited a higher antimicrobial activity against the planktonic Gram-positive Staphylococcus aureus and Bacillus subtilis strains and the Candida albicans fungal strain. The obtained compounds also inhibited the ability of S. aureus , B. subtilis , Escherichia coli and C. albicans strains to colonize the inert substratum, accounting for their possible use as antibiofilm agents. All the active compounds exhibited low or acceptable cytotoxicity levels on the HCT8 cells, ensuring the potential use of these compounds for the development of new antimicrobial drugs with minimal side effects on the human cells and tissues.- Published
- 2020
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33. The Dermoscopic Rainbow Pattern - A Review of the Literature.
- Author
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Draghici C, Vajaitu C, Solomon I, Voiculescu VM, Popa MI, and Lupu M
- Subjects
- Humans, Color, Dermoscopy, Skin Diseases pathology
- Abstract
The "rainbow" pattern is a relatively new dermoscopic term that describes a bluish-reddish coloration together with various colors of the rainbow observable mainly through polarized light dermoscopy. Despite several theories, the rainbow pattern has not yet been clearly associated with any particular histological structure. This feature has been described in skin lesions with abundant vascularization such as Kaposi's sarcoma, basal cell carcinoma, scars, squamous cell carcinoma, melanoma, and others. In this paper we conducted a review of the available studies regarding the appearance of the rainbow pattern in different pathologies. Furthermore, we present a detailed description of the physical phenomenon in order to obtain a better understanding of this peculiar dermoscopic feature.
- Published
- 2019
34. The impact of lifestyle factors on evolution of atopic dermatitis: An alternative approach.
- Author
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Solomon I, Ilie MA, Draghici C, Voiculescu VM, Căruntu C, Boda D, and Zurac S
- Abstract
Atopic dermatitis (AD) is a multifactorial chronic inflammatory disease with an incompletely understood etiopathogenesis. With a significant impact on the quality of life of patients, AD has attracted the interest of many research studies aiming to investigate the complex cellular and molecular mechanisms and to identify new therapeutic pathways. Various studies have focused on psycho-immunology, emphasizing the involvement of stress, defined as a general response of the body to external or internal challenges to the AD pathology. Factors like lifestyle and leisure activities may change the behavior of immune cells in AD with a strong impact on the evolution of the disease. Moreover, the poor adherence of AD patient to standard treatment approach has led to the necessity to combine different therapies in the field of complementary and alternative medicine. Although there are still not enough data to conclude that adjuvant therapies are effective in a conventional sense, there are already promising results suggesting that alternative therapeutic strategies could be a main subject of further research.
- Published
- 2019
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35. Coexistence of Psoriasis, Vitiligo and Oral Lichen Planus – a New Variant of Multiple Autoimmune Syndrome?
- Author
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Vajaitu C, Voiculescu VM, Draghici C, Solomon I, and Lupu M
- Published
- 2018
- Full Text
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36. Biomimetic Planar Polymer Membranes Decorated with Enzymes as Functional Surfaces.
- Author
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Draghici C, Mikhalevich V, Gunkel-Grabole G, Kowal J, Meier W, and Palivan CG
- Subjects
- Adsorption, Biomimetics, Laccase chemistry, Monophenol Monooxygenase chemistry, Surface Properties, Wettability, Laccase metabolism, Membranes, Artificial, Monophenol Monooxygenase metabolism, Polymers chemistry, Water Purification methods
- Abstract
Functional surfaces were generated by a combination of enzymes with polymer membranes composed of an amphiphilic, asymmetric block copolymer poly(ethyleneglycol)- block-poly(γ-methyl-ε-caprolactone)- block-poly[(2-dimethylamino)ethylmethacrylate]. First, polymer films formed at the air-water interface were transferred in different sequences onto silica solid support using the Langmuir-Blodgett technique, generating homogeneous monolayers and bilayers. A detailed characterization of these films provided insight into their properties (film thickness, wettability, topography, and roughness). On the basis of these findings, the most promising membranes were selected for enzyme attachment. Functional surfaces were then generated by the adsorption of two model enzymes that can convert phenol and its derivatives (laccase and tyrosinase), well known as high-risk pollutants of drinking and natural water. Both enzymes preserved their activity upon immobilization with respect to their substrates. Depending on the properties of the polymer films, different degrees of enzymatic activity were observed: bilayers provided the best conditions in terms of both overall stability and enzymatic activity. The interaction between amphiphilic triblock copolymer films and enzymes is exploited to engineer "active surfaces" with specific functionalities and high efficacy resulting from the intrinsic activity of the biomolecules that is preserved by an appropriate synthetic environment.
- Published
- 2018
- Full Text
- View/download PDF
37. Sydnone C-4 heteroarylation with an indolizine ring via Chichibabin indolizine synthesis.
- Author
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Albota F, Caira MR, Draghici C, Dumitrascu F, and Dumitrescu DE
- Abstract
The synthesis of sydnones heteroarylated at C-4 with an indolizine was achieved by Chichibabin (Tschitschibabin) indolizine synthesis starting from the corresponding sydnone- N -pyridinium bromides. The latter compounds were also transformed to sydnone-indolizines connected through a keto group at the C-4 position by refluxing them in 1,2-epoxybutane with an activated alkyne. The structures of the new compounds were assigned by FTIR, NMR spectroscopy and X-ray analysis.
- Published
- 2016
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38. Concise total synthesis of glucosepane.
- Author
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Draghici C, Wang T, and Spiegel DA
- Subjects
- Amino Acids chemistry, Glucose chemistry, Humans, Imidazoles chemical synthesis, Proteins chemistry, Proteins metabolism, Glycation End Products, Advanced chemical synthesis, Protein Processing, Post-Translational
- Abstract
Glucosepane is a structurally complex protein posttranslational modification that is believed to exist in all living organisms. Research in humans suggests that glucosepane plays a critical role in the pathophysiology of both diabetes and human aging, yet comprehensive biological investigations of this metabolite have been hindered by a scarcity of chemically homogeneous material available for study. Here we report the total synthesis of glucosepane, enabled by the development of a one-pot method for preparation of the nonaromatic 4H-imidazole tautomer in the core. Our synthesis is concise (eight steps starting from commercial materials), convergent, high-yielding (12% overall), and enantioselective. We expect that these results will prove useful in the art and practice of heterocyclic chemistry and beneficial for the study of glucosepane and its role in human health and disease., (Copyright © 2015, American Association for the Advancement of Science.)
- Published
- 2015
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39. Synthesis and apoptotic activity of new pyrazole derivatives in cancer cell lines.
- Author
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Nitulescu GM, Draghici C, Olaru OT, Matei L, Ioana A, Dragu LD, and Bleotu C
- Subjects
- Apoptosis, Cell Line, Tumor, Humans, Pyrazoles chemical synthesis, Pyrazoles chemistry
- Abstract
We designed and synthesized new pyrazole thiourea chimeric derivatives and confirmed their structures by NMR and IR spectra. Apoptotic effects were studied in human cancer cells. The N-[(1-methyl-1H-pyrazol-4-yl)carbonyl]-N'-(3-bromophenyl)-thiourea compound (4b) exhibited the highest apoptosis-inducing effect. Compound 4b and the thiazole derivatives, 5b and 6b, increased the expression of tumor necrosis factor receptors TRAIL-R2 and TRAIL-R1, accompanied by down-modulation of pro-caspase 3 levels, and the augmentation of cleaved caspase 3. They also reduced the levels of apoptosis inhibitory proteins and the expression of the heat-shock proteins Hsp27 and Hsp70. All the tested pyrazole derivatives induced a concentration-dependent increase of cells in G2/M phases. The analysis of the experimental data indicates the reduction of Akt phosphorylation as the most probable cellular mechanism of action for the tested compounds. The in vitro study indicated that compound 4b could be a promising anti-cancer drug, to be further developed in animal models of cancer., (Copyright © 2015 Elsevier Ltd. All rights reserved.)
- Published
- 2015
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40. Indolizines and pyrrolo[1,2-c]pyrimidines decorated with a pyrimidine and a pyridine unit respectively.
- Author
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Popa MM, Georgescu E, Caira MR, Georgescu F, Draghici C, Stan R, Deleanu C, and Dumitrascu F
- Abstract
The three possible structural isomers of 4-(pyridyl)pyrimidine were employed for the synthesis of new pyrrolo[1,2-c]pyrimidines and new indolizines, by 1,3-dipolar cycloaddition reaction of their corresponding N-ylides generated in situ from their corresponding cycloimmonium bromides. In the case of 4-(3-pyridyl)pyrimidine and 4-(4-pyridyl)pyrimidine the quaternization reactions occur as expected at the pyridine nitrogen atom leading to pyridinium bromides and consequently to new indolizines via the corresponding pyridinium N-ylides. However, in the case of 4-(2-pyridyl)pyrimidine the steric hindrance directs the reaction to the pyrimidinium N-ylides and, subsequently, to the formation of the pyrrolo[1,2-c]pyrimidines. The new pyrrolo[1,2-c]pyrimidines and the new indolizines were structurally characterized through NMR spectroscopy. The X-ray structures of two of the starting materials, 4-(2-pyridyl)pyrimidine and 4-(4-pyridyl)pyrimidine, are also reported.
- Published
- 2015
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41. Synthetic Approaches and Total Syntheses of Vinigrol, a Unique Diterpenoid.
- Author
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Draghici C and Njardarson JT
- Abstract
This review summarizes all published total and formal syntheses as well as synthetic approaches towards vinigrol. The content is divided into sections, which are focused on each research groups contributions and how far each approach was advanced towards vinigrol. Graphical summaries of all the published vinigrol structural perspectives, starting materials used for each routes and a discussion of preferred or privileged reactions employed is also presented.
- Published
- 2015
- Full Text
- View/download PDF
42. Design, Synthesis, Characterization and Antimicrobial Evaluation of Some Heterocyclic Condensed Systems with Bridgehead Nitrogen from Thiazolotriazole Class.
- Author
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Barbuceanu SF, Draghici C, Barbuceanu F, Bancescu G, and Saramet G
- Subjects
- Anti-Bacterial Agents chemical synthesis, Anti-Bacterial Agents chemistry, Antifungal Agents chemical synthesis, Antifungal Agents chemistry, Candida drug effects, Dose-Response Relationship, Drug, Gram-Negative Bacteria drug effects, Gram-Positive Bacteria drug effects, Heterocyclic Compounds chemical synthesis, Heterocyclic Compounds chemistry, Microbial Sensitivity Tests, Molecular Structure, Nitrogen chemistry, Structure-Activity Relationship, Thiazoles chemistry, Triazoles chemistry, Anti-Bacterial Agents pharmacology, Antifungal Agents pharmacology, Drug Design, Heterocyclic Compounds pharmacology, Thiazoles pharmacology, Triazoles pharmacology
- Abstract
In the present study, a series of new heterocyclic condensed systems with bridgehead nitrogen from the thiazolo[3,2-b][1,2,4]triazoles class was synthesized starting from some 4-(4-X-phenylsulfonyl)phenyl)-4H-1,2,4-triazole-3-thioles 1a-c (X=H, Cl, Br). The intermediates of S-alkylated 1,2,4-triazoles, 2-(5-(4-(4-X-phenylsulfonyl)phenyl)-2H-1,2,4-triazol-3-ylthio)-1-(4-fluorophenyl)ethanones 2a-c, were obtained by treatment of triazoles 1a-c with 2-bromo-4'-fluoroacetophenone. The 2-(4-(4-X-phenylsulfonyl)phenyl)-6-(4-fluorophenyl)thiazolo[3,2-b][1,2,4]triazoles 3a-c were obtained by cyclization of S-alkylated 1,2,4-triazoles 2a-c in sulfuric acid media, at 0 °C. For the synthesis of 2-(4-(4-X-phenylsulfonyl)phenyl)-5-(4-fluorobenzylidene)-thiazolo[3,2-b][1,2,4]triazol-6(5H)-ones 4a-c, the triazoles 1a-c were treated with 4-fluorobenzaldehyde, chloroacetic acid and anhydrous sodium acetate, in the presence of acetic acid and acetic anhydride. The structures of the newly synthesized compounds have been confirmed by elemental analysis and spectral methods (IR, 1H-NMR, 13C-NMR, MS). The antimicrobial activity of all new compounds has been screened against some bacteria and yeasts.
- Published
- 2015
- Full Text
- View/download PDF
43. "Active surfaces" formed by immobilization of enzymes on solid-supported polymer membranes.
- Author
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Draghici C, Kowal J, Darjan A, Meier W, and Palivan CG
- Subjects
- Adsorption, Air, Enzymes, Immobilized metabolism, Hydrophobic and Hydrophilic Interactions, Laccase chemistry, Laccase metabolism, Models, Molecular, Protein Conformation, Silicon Dioxide chemistry, Trametes enzymology, Water chemistry, Wettability, Enzymes, Immobilized chemistry, Membranes, Artificial, Methacrylates chemistry, Nylons chemistry, Polyesters chemistry, Polyethylene Glycols chemistry
- Abstract
In various domains ranging from catalysis to medical and environmental sciences, there is currently much focus on the design of surfaces that present active compounds at the interface with their environments. Here, we describe the design of "active surfaces" based on solid-supported monolayers of asymmetric triblock copolymers, which serve as templates for the attachment of enzymes. A group of poly(ethylene glycol)-block-poly(γ-methyl-ε-caprolactone)-block-poly[(2-dimethylamino) ethyl methacrylate] amphiphilic copolymers, with different hydrophilic and hydrophobic domains (PEG45-b-PMCLx-b-PDMAEMAy) was selected to generate solid-supported polymer membranes. The behavior of the copolymers in terms of their molecular arrangements at the air-water interface was established by a combination of Langmuir isotherms and Brewster angle microscopy. Uniform thin layers of copolymers were obtained by transferring films onto silica solid supports at optimal surface pressure. These solid-supported polymer membranes were characterized by assessing various properties, such as monolayer thickness, hydrophilic/hydrophobic balance, topography, and roughness. Laccase, used as an enzyme model, was successfully attached to copolymer membranes by stable interactions as followed by quartz crystal microbalance with dissipation measurements, and its activity was preserved, as indicated by activity assays. The interaction between the amphiphilic triblock copolymer films and immobilized enzymes represents a straightforward approach to engineer "active surfaces", with biomolecules playing the active role by their intrinsic bioactivity.
- Published
- 2014
- Full Text
- View/download PDF
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