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Treatment for microbial infections still remains an important health problem for researchers around the world. Despite a broad range of antimicrobial drugs today, there are certain obstacles associated with the use of antimicrobial agents such as drug resistance and toxicity. Thus, medicinal chemists concentrate on designing novel antimicrobial drugs. In the search for new antimicrobial agents; 1,3,4-oxadiazole compounds have come forward due to their hydrolytic stability, good chemical and thermal stability. In the scope of this work, 2-(6-chloropyridin-3-yl)-5-(substitutedphenyl)-1,3,4-oxadiazole (4a–4i) were synthesizedusing 6-chloro-N'-(substitutedbenzoyl)nicotinohydrazide (3a–3i). These compounds were screened for their antimicrobial activities against as gram-positive bacteria S. aureus, E. faecalis, as gram-negative bacteria E. coli, P. aeruginosa, as yeast C. parapsilosis, C. albicans, C. glabrata. Among the 1,3,4-oxadiazole compounds, 4h against E. faecalis and 4b, 4f and 4g against E. coli have been found to exhibit as much as potency chloramphenicol with MIC50 values of 62.50 µg/mL.

Karaca, Hulya/0000-0002-6578-1341; Kubilay, Aslihan/0000-0002-6979-4932, WOS: 000531981900001, Some new 3,4,5-trisubstituted 1,2,4-triazole derivatives were synthesized and studied for their antimicrobial activity. the lead compounds were obtained starting from 8-hydroxyquinoline and ethyl 2-chloroacetate. the obtained ester compound (1) first reacted with hydrazine hydrate (2) then with phenyl isothiocyanate (3). Ring closure by KOH led to 3-mercapto-1,2,4-triazole derivative (4). Lastly, it reacted with 2-chloro-N-(substituted (benzo)/thiazole)acetamide derivatives to obtain the final compounds (5a-j). the structural elucidation of the compounds was performed by H-1 NMR and C-13 NMR spectroscopy and high resolution mass spectrometry techniques and elemental analysis. the synthesized compounds were investigated for their antimicrobial activities against seven bacteria and four fungi. As a result of the activity studies, it was observed that compounds N-(6-nitrobenzothiazol-2-yl)-2-[[4-phenyl-5-((quinolin-8-yloxy)methyl)-4H-1,2,4-triazol-3-yl]thio]acetamide (5a) and N-(6-fluorobenzothiazol-2-yl)-2-[[4-phenyl-5-((quinolin-8-yloxy)methyl)-4H-1,2,4-triazol-3-yl]thio]acetamide (5d) were the most active molecules. Also, the antifungal activity of the compounds was found to be higher than their antibacterial activity although lower than the standard drug's potential. Additionally, the physicochemical properties of the compounds were calculated which were evaluated to be at a suitable range for oral administration.

Wastewater from the textile industry contaminated with azo dyes affects the environment negatively, causes pollution, and threatens environmental balance. Among various methods for wastewater treatment, bioremediation emerges as an environmentally friendly, economical, and sustainable solution. In this study, white-rot fungus Sporotrichum sp. was employed to decolorize reactive blue 13 (RB13). The long-term decolorization capacity of the fungus was investigated by a sequential batch experiment under optimized conditions. The fungus showed high decolorization efficiency upon repeating usage, and its decolorization efficiency decreased from 97.4% to 87.09% after transferring to a freshly prepared medium seven times. The MTT (3-(4, 5-dimethylthiazolyl-2)-2, 5-diphenyltetrazolium bromide) assay) method using Chinese Hamster Lung V79 379A was performed to assess the cytotoxicity of treated water samples. This study revealed that Sporotrichum sp. has short-term enzymatic and long-term biosorption capacity on reactive blue 13 and the decolorization potential of the alive and dead cells is impressively high. PRACTITIONER POINTS: White-rot fungus Sporotrichum sp. is able to decolorize sulfonated azo-dye reactive blue 13 upon sequential incubation in freshly prepared dye solution. The decolorization mechanism of the fungus is estimated to be bioadsorption. Sporotrichum sp. can be considered for long-term usage and immobilization applications.

WOS: 000433998700006, Background: Pyrazolines have played a pivotal role in antimicrobial and anticancer drug discovery. Moreover, thiazoles have attracted a great deal of interest due to their crucial roles in the lead identification and optimization. Objectives: The purpose of the current work was to design and synthesize new antimicrobial and anticancer agents. Methods: New thiazolyl-pyrazoline derivatives (2a-d) were synthesized via the ring closure reaction of 3-(2-thienyl)-5-(2,6-dichlorophenyl)-1-thiocarbamoyl-2-pyrazoline (1) with phenacyl bromides. The compounds were evaluated for their in vitro antimicrobial effects on pathogenic bacteria and Candida species using Microdilution assay, BacTiter-Glo (TM) microbial cell viability assay and Fluorescence microscopy. The possible binding interactions of compound 1 in the active site of CYP51 were confirmed by molecular docking studies, whereas its genotoxicity was investigated using Ames MPF test. Furthermore, MTT assay was performed to determine the cytotoxic effects of the compounds on A549 human lung adenocarcinoma, HepG2 human hepatocellular carcinoma, C6 rat glioma, and NIH/3T3 mouse embryonic fibroblast cell lines. A computational study for the prediction of ADME properties of all compounds was also performed. Results: Compound 1 was found to be the most potent anticandidal agent against Candida species. MTT and Ames MPF assays indicated that compound 1 was neither cytotoxic nor genotoxic at the concentrations tested. Docking studies showed that compound 1 interacted with Heme group in the active site of CYP51. This compound also exhibited selective anticancer activity against HepG2 and C6 cell lines. According to in silico studies, this compound did not violate Lipinski's rule, making it a potential orally bioavailable chemotherapeutic agent. Conclusion: Compound 1 was identified as a promising candidate for further mechanistic studies., Anadolu University Scientific Research Projects Commission [1604S158], This study was supported by Anadolu University Scientific Research Projects Commission under the grant no: 1604S158.

Antidepressants are drugs commonly used in clinical settings. However, there are very limited studies on the effects of these drugs on the gut microbiota. Herein, we evaluated the effect of reboxetine (RBX), a selective norepinephrine (noradrenaline) reuptake inhibitor (NRI), on gut microbiota in both diabetic and non-diabetic rats. This is the first report of relation between reboxetine use and the gut microbiota to our knowledge. In this study, type-1 diabetes induced by using streptozotocin (STZ) and RBX was administered to diabetic rats and healthy controls for 14 days. At the end of the treatment, stool samples were collected. Following DNA extraction, amplicon libraries for the V3-V4 region were prepared and sequenced with the Illumina Miseq platform. QIIME was used for preprocessing and analysis of the data. As a result, RBX had a significant effect on gut microbiota structure and composition in diabetic and healthy rats. For example, RBX exposure had a pronounced microbial signature in both groups, with a low Firmicutes/Bacteroidetes ratio and low Lactobacillus levels. While another abundance phylum after exposure to RBX was Proteabacteria, other notable taxa in the diabetic group included Flavobacterium, Desulfovibrionaceae, Helicobacteriaceae, Campylobacterales, and Pasteurellacae when compared to the untreated group.

WOS: 000404248000004, PubMed ID: 28561221, Looking for new cytotoxic and antimicrobial agents with improved antitumor activity, a series of hydrazide and oxadiazole derivatives were designed and synthesized using 3-methoxyphenol as starting substance. Novel N'-(arylidene)-2-(3-methoxyphenoxy) acetohydrazide derivatives (4a-f) / 1-(4-substitutedphenyl)-2-[(5-[(3-methoxyphenoxy) methyl]1,3,4- oxadiazol-2-yl) thio] ethan-1-one derivatives (6a-f)/N-(6-substitutedbenzothiazol-2-yl)-2-[(5-[(3-methoxyphenoxy) methyl]-1,3,4-oxadiazol-2-yl) thio] acetamide derivatives (7a-e) were obtained and evaluated for their in vitro antimicrobial activity against various gram-positive, gram-negative bacteria and fungi. The antimicrobial activity potential of the compounds against gram-negative bacteria was found to have higher compared to the potential against gram-positive bacteria. Also, compounds were screened for their antiproliferative activity against 2 selected human tumor cell lines, A549 lung, MCF7 breast cancer cell line and mouse embryo fibroblast cell line, NIH/3T3 as healthy cell line. Among the compounds evaluated, compound 7c bearing 1,3,4-oxadiazole ring and 6-methoxy benzothiazole moiety exhibited the highest inhibitory activity against A549 and MCF-7 tumor cell lines in contrary to NIH/3T3 cell line, as desired.

WOS: 000482452000006, A series of 2-(substituteddithiocarbamoyl)-N-[4-((1H-imidazol-1-yl)methyl)phenyl]acetamide derivatives was designed and synthesized to combat the increasing incidence of drug-resistant fungal infections. All synthesized compounds were characterized by IR, H-1-NMR, C-13-NMR, and HRMS spectra and elemental analyses. Antifungal activity tests were performed against four different fungal strains. Molecular docking studies were performed to investigate the mode of action towards the fungal lanosterol 14 alpha-demethylase, a cytochrome P450-dependent enzyme. ADME studies were carried out and a connection between activities and physicochemical properties of the target compounds was determined. Most of the final compounds exhibited significant activity against Candida albicans and Candida krusei with MIC50 value 12.5 mu g/mL. The results of in vitro anti-Candida activity, a docking study and ADME prediction revealed that the newly synthesized compounds have potential anti-Candida activity and evidenced the most active derivative, 5b (2-Pyrrolidinthiocarbonylthio-N-[4-((1H-imidazol-1-yl)methyl)phenyl]acetamide), which can be further optimized as a lead compound.

10 yeni kinoksalin hidrazondan oluşan yeni bir grup aktimikrobiyal aktivitesi incelenmek üzere sentezlenmiştir. Bileşiklerin yapıları IR, 1H-NMR, MS spektral ve elemental analiz ile aydınlatılmıştır. Bileşiklerin antimikrobiyal aktiviteleri Mikro-broth dilüsyon yöntemi ile 3 fungus ve 7 bakteri türüne karşı değerlendirilmiştir. Sentezlenen bütün bileşikler Pseudomonas aeruginosa’ ya karşı önemli antibakteriyal aktivite göstermiştir. Ayrıca, 2,4-difloro yapısı içeren 4b bileşiği Pseudomonas aeruginosa’ ya karşı kloramfenikolden 2 kat daha iyi antibakteriyal aktivite göstermiştir

WOS: 000388251200005, PubMed ID: 30475497, The synthesis of nine new quinazoline derivatives (2a-21) and evaluation of their antimicrobial and cytotoxic activities were aims of the present work. For the synthesis of the compounds, 2-chloro-6,7-dimethoxyquinazolin-4-amine was used as the initial starting material. The intermediate product, 2-hydrazinyl-6,7-dimethoxyquinazolin-4-amine, was reacted with appropriate aromatic aldehydes to obtain 2-(2-benzylidenehydrazinyl)-6,7-dimethoxyquinazolin-4-amine derivatives as final compounds. The structures of the compounds were elucidated by and C-13-NMR, IR, and MS analyses. The new pure compounds were evaluated for their potential antimicrobial and cytotoxic activities using in vitro microdilution and cell culture techniques, respectively. The compounds 2e and 2f may be promising candidates for the treatment of fungal infections with their activity and cytotoxicity.

WOS: 000443379600008, PubMed ID: 30079557, 1,3-Oxazolidine-2-one is an important heterocyclic ring participating in the chemical structure of many drugs. In this research, 22 new amide/sulfonamide/thiourea derivatives (1-22) were obtained by the reaction of (S)-4-(4-aminobenzyl)-2(1H)-1,3-oxazolidinone with 4-substituted benzoyl chlorides, 4-substituted benzene sulfonyl chlorides, and 4-substituted phenyl isothiocyanates. The structures of all synthesized compounds were clarified by FT-IR, NMR, and mass spectroscopic and elemental analysis techniques. The synthesized compounds were screened for their antimicrobial activity. Antimicrobial susceptibility and cellular physiology were evaluated using the microbroth dilution assay and the flow cytometry method. As a result, it was determined that compound 16 displayed better antimicrobial activity than chloramphenicol against Gram-positive bacteria, especially Staphylococcus aureus. In order to understand the mechanism of effect of the compounds on the cell membrane, fluorescence microscopy was used. Cell membrane damage of the Gram positive bacteria treated with compound 16 was observed as a result of intense staining with propidium iodide. In addition, genotoxicity, cytotoxicity, and absorption, distribution, metabolism, and excretion (ADME) parameters of compound 16 were examined and it was found as non-mutagenic and non-cytotoxic at the concentration at which it showed antimicrobial activity. According to the calculated ADME parameters and drug likeness scores, the compounds can be good drug candidates, especially compound 16.

WOS: 000357471400001, New 2-(4-arylpiperazine-1-yl)-N-[4-(2-(4-substituted phenyl)thiazol-4-yl)phenyl]acetamide derivatives were synthesized and evaluated for their antimicrobial and anticholinesterase activities. Acetylcholinesterase inhibitory activities of the compounds were found weak contrary to expectations. It is unlikely that antifungal activity of the compounds was found significant, especially against Candida parapsilosis., Anadolu University Scientific Research Project, Eskisehir, Turkey [1505S407], The study was supported by the Anadolu University Scientific Research Project, Eskisehir, Turkey (Project no. 1505S407). The authors present their thanks to Anadolu University Medicinal Plants, Drugs and Scientific Research Center (AUBIBAM) for NMR analyses. The assistance of the staff is gratefully appreciated.

WOS: 000419242400081, PubMed ID: 29189730, In an effort to develop new potent antimicrobial and anticancer agents, new pyrrole-based chalcones were designed and synthesized via the base-catalyzed Claisen-Schmidt condensation of 2-acetyl-1-methylpyrrole with 5-(aryl)furfural derivatives. The compounds were evaluated for their in vitro antimicrobial effects on pathogenic bacteria and Candida species using microdilution and ATP luminescence microbial cell viability assays. MTT assay was performed to determine the cytotoxic effects of the compounds on A549 human lung adenocarcinoma, HepG2 human hepatocellular carcinoma, C6 rat glioma, and NIH/3T3 mouse embryonic fibroblast cell lines. 1-(1-Methyl-1H-pyrrol-2-yl)-3-(5-(4-chlorophenyl)furan-2-yl)prop-2-en-1-one (7) and 1-(1-methyl-1H-pyrrol-2-yl)-3-(5-(2,5-dichlorophenyl)furan-2-yl)prop-2-en-1-one (9) were found to be the most potent antifungal agents against Candida krusei and therefore these compounds were chosen for flow cytometry analysis and Ames MPF assay. ATP bioluminescence assay indicated that the antifungal activity of compounds 7 and 9 against C. krusei was significantly higher than that of other compounds and the reference drug (ketoconazole), whereas flow cytometry analysis revealed that the percentage of dead cells treated with compound 7 was more than that treated with compound 9 and ketoconazole. According to Ames MPF assay, compounds 7 and 9 were found to be non-genotoxic against TA98 and TA100 with/without metabolic activation. MTT assay indicated that 1-(1-methyl-1H-pyrrol-2-yl)-3-(5-(2-nitrophenyl)furan-2-yl)prop-2-en-1-one (3) showed more selective anticancer activity than cisplatin against the HepG2 cell line. On the other hand, 1-(1-methyl-1H-pyrrol-2-yl)-3-(5-(4-nitrophenyl)furan-2-yl)prop-2-en-1-one (1) was found to be more effective and selective on the A549 cell line than cisplatin., Anadolu University Scientific Research Projects Commission [1605S488, 1705S166], This study was supported by the Anadolu University Scientific Research Projects Commission under the grant numbers: 1605S488 and 1705S166.

WOS: 000399579300016, PubMed ID: 28413890, A series of 2-(4-substitutedmethylphenyl) propionic acid derivatives (6a-6m) were synthesized, characterized and evaluated for cyclooxygenase (COX) enzyme inhibitory and antimicrobial activity. Test compounds that exhibited good COX inhibition and antibacterial activity were further screened for their cytotoxicity and genotoxicity. Compounds 6h and 6l showed better COX-1 and COX-2 inhibition when compared to ibuprofen. Inhibition potency of these compounds against COX-2 was very close to that of nimesulide. The compounds 6d, 6h, 6l and 6m displayed promising antibacterial property when compared to chloramphenicol. However, the compound 6l was emerged as the best dual COX inhibitory-antibacterial agent in this study. The ADME prediction of the compounds revealed that they may have a good pharmacokinetic profile. Docking results of the compounds 6h and 6l with COX-1 (PDB ID: 1EQG) also exhibited a strong binding profile., Anadolu University Scientific Projects Fund [1409S385], This study was financially supported by Anadolu University Scientific Projects Fund, Project No: 1409S385.

WOS: 000395967900011, PubMed ID: 28174104, Owing to the growing need for novel antibacterial agents, we synthesized a novel series of fluoroquinolones including 7-substituted-1-(2,4-difluoropheny1)-6-fluoro-4-oxo-1,4-dihydro[1,8]naphthyridine-3-carboxylic acid derivatives, which were tested against clinically relevant Gram positive and Gram negative bacteria. Chemical structures of the synthesized compounds were identified using spectroscopic methods. In vitro antimicrobial effects of the compounds were determined via microdilution assay. Microbiological examination revealed that compounds 13 and 14 possess a good antibacterial profile. Compound 14 was the most active and showed an antibacterial profile comparable to that of the reference drugs trovafloxacin, moxifloxacin, and ciprofloxacin. A significant MIC90 value (1.95 mu g/mL) against S. aureus ATCC 25923, E. coli ATCC 35218, and E. coli ATCC 25922 was recorded for compound 14. We observed reduced metabolic activity associated with compounds 13 and 14 in the relevant bacteria via a luminescence ATP assay. Results of this assay supported the antibacterial potency of compounds 13 and 14. An E. coli DNA gyrase inhibitory assay indicated that compound 14 is a potent inhibitor of E. coli DNA gyrase. Docking studies revealed that there is a strong interaction between compound 14 and the E. coli DNA gyrase enzyme. Genotoxicity and cytotoxicity evaluations of compounds 13 and 14 showed that compound 14 is non-genotoxic and less cytotoxic compared to the reference drugs (trovafloxacin, moxifloxacin, and ciprofloxacin), which increases its biological importance, Anadolu University Scientific Projects Fund [16055290], This study was financially supported by Anadolu University Scientific Projects Fund, Project No.: 16055290. Authors are thankful to Ms. Begfim Nurpelin Saglik for help with the docking study.

Değişen dünya eğilimlerine bağlı olarak renkli ürünlere olan ilgi artmaktadır. Tekstil endüstrisinde kumaşlara mavi rengi vermek amacı ile Ambifiks Blue H5R (Blue 13) boyası yoğun bir şekilde kullanılmaktadır. Bu boyanın fabrikalardan çevredeki alıcı sulara verilmesi sonucu çeşitli toksik etkiler oluşmaktadır. Bu toksik etkileri indirgemek amacı ile Porsuk Çayından izole edilmiş Aspergillus niveus 2 ve Fusarium moniliforme’ nin bu boyayı farklı fizyolojik koşullarda (pH, sıcaklık, çalkalama koşulları) renk giderimi yetenekleri araştırılmıştır. A. niveus için pH 3, 35OC ve 120-150 rpm de % 95 e varan sonuçlar elde edilirken, F. moniliforme için pH 7, 20 OC ve 120 rpm de % 95 e varan sonuçlar elde edilmiştir. A. niveus için ölü ve canlı hücrelerin renk giderim sonuçları yakınken, F. moniliforme için ölü hücrelerin renk giderimi %90 larda canlı hücrelerin ise % 75 lerdedir

A new class of 10 novel quinoxaline hydrazones was synthesized to examine their antimicrobial activity. The structural of the compounds was confirmed by IR, 1H-NMR, and MS spectral data and elemental analyses. Antimicrobial activity of the compounds was evaluated against 3 fungal and 7 bacterial strains by Micro-broth dilution assay. All of the synthesized compounds indicated showed significant antibacterial activity against Pseudomonas aeruginosa. Furthermore, antibacterial activity of the 2,4-difluoro substituted compound 4b displayed two fold better activity than chloramphenicol against this bacterial strain., 10 yeni kinoksalin hidrazondan oluşan yeni bir grup aktimikrobiyal aktivitesi incelenmek üzere sentezlenmiştir. Bileşiklerin yapıları IR, 1H-NMR, MS spektral ve elemental analiz ile aydınlatılmıştır. Bileşiklerin antimikrobiyal aktiviteleri Mikro-broth dilüsyon yöntemi ile 3 fungus ve 7 bakteri türüne karşı değerlendirilmiştir. Sentezlenen bütün bileşikler Pseudomonas aeruginosa’ ya karşı önemli antibakteriyal aktivite göstermiştir. Ayrıca, 2,4-difloro yapısı içeren 4b bileşiği Pseudomonas aeruginosa’ ya karşı kloramfenikolden 2 kat daha iyi antibakteriyal aktivite göstermiştir

WOS: 000303471900027, In this study, the antimicrobial activities of Trimethoprim (1), Trimethoprim + Maleic acid (2), Trimethoprim + Oxalic acid dihydrate (3), and Trimethoprim + trans-1,2-Cyclohexanedicarboxylic acid (4) were investigated for their in vitro growth inhibitory activity against human pathogenic as some bacteria and fungi. Substances were tested using the micro-broth dilution assay. The chemical agents showed the same activity against Escherichia coli, Pseudomonas aeruginosa, and Proteus vulgaris. Inhibitory activities of test chemicals against different Candida strains were determined to be widely moderate., Anadolu University, Commission of Scientific Research Projects, Authors are grateful to Anadolu University, Commission of Scientific Research Projects for support of this study.

WOS: 000289418300008, PubMed ID: 21469176, In the present study a new series of benzimidazole derivatives bearing various (benz)azolylthio moieties were synthesized so as to investigate their antimicrobial activity. Structures of the target compounds (5a-5i) were confirmed by their IR, (1)H-NMR, ES-MS spectral data, and elemental analyses. The synthesized compounds (5a-5i) exhibited poor activity against bacterial strains. On the other hand, antifungal activity of the compounds against Candida species was very significant. Brine-Shrimp lethality assay was performed for determination of toxicity of the compounds. Compounds 5a, 5c, and 5d were evaluated as non-toxic in addition to their attractive antifungal activity. However, the other compounds (5b, e-i) in the series showed toxicity to different extents.

WOS: 000344693400001, 18 novel dithiocarbamate derivatives were synthesized in order to investigate their inhibitory potency on acetylcholinesterase enzyme and antimicrobial activity. Structures of the synthesized compounds were elucidated by spectral data and elemental analyses. The synthesized compounds showed low enzyme inhibitory activity. However, they displayed good antimicrobial activity profile. Antibacterial activity of compounds 4a, 4e, and4p (MIC= 25 mu g/mL) was equal to that of chloramphenicol against Klebsiella pneumoniae (ATCC 700603) and Escherichia coli (ATCC 35218). Most of the compounds exhibited notable antifungal activity against Candida albicans (ATCC 10231), Candida glabrata (ATCC 90030), Candida krusei (ATCC 6258), and Candida parapsilosis (ATCC 7330). Moreover, compound 4a, which carries piperidin-1-yl substituent and dimethylthiocarbamoyl side chain as variable group, showed twofold better anticandidal effect against all Candida species than reference drug ketoconazole., Anadolu University Scientific Research Projects Fund [1205S88], This study was financially supported by Anadolu University Scientific Research Projects Fund, project no. 1205S88.

WOS: 000318995000002, Some benzimidazole derivatives bearing hydrazone moiety were synthesized and their in vitro antimicrobial activity was determined against various gram-positive and gram-negative bacteria, and fungi using microbroth dilution method. The structures of all new compounds were identified by H-1-NMR, FT-IR, MS spectroscopic techniques and elemental analysis. Sixteen final products were examined for their in vitro antimicrobial activities. When compared to the reference agents, chloramphenicol and ketoconazole, most of the synthesized compounds showed sufficient antibacterial activity against Pseudomonas aeruginosa and antifungal activity against Candida albicans and C. glabrata.

WOS: 000312874100022, In the present study, some isoxazole-(benz)azole derivatives (3a-3j) were synthesized by considering antimicrobial and anticancer potencies of azole compounds. Chemical structures of obtained compounds (3a-3j) were confirmed by the data of spectral and elemental analyses. Anticancer activity evaluation was performed at two steps. Initially, cytotoxic effects of the compounds (3a-3j) on HT-29 (colon carcinoma) and C-6 (melanoma) cell lines were determined by MTT assay. Secondly, the compounds 3g-3i, which indicated significant cytotoxicity were selected and analysed for their inhibitory activity on DNA synthesis of carcinogenic cells. The compounds 3g and 3h showed notable DNA synthesis inhibition on both cancer cell lines. Antibacterial and antifungal activities of the synthesized compounds (3a-3j) were also examined. All of the compounds exhibited very poor antibacterial activity against gram negative and gram positive bacterial strains, whereas antifungal activity of the compounds 3a-3f was equal to that of Ketoconazole.

WOS: 000321693400024, PubMed ID: 22651798, In this work, we synthesized fourteen different compounds which contain hydrazone bridged thiazole and pyrrole rings. For this purpose, pyrrole-2-carboxaldehydes were reacted directly with thiosemicarbazide in ethanol and then obtained thiosemicarbazones were condensed with alpha-bromoacetophenone derivatives (Hantzsch reaction) to give 1-substituted pyrrole-2-carboxaldehyde [4-(4-substituted phenyl)-1,3-thiazol-2-yl] hydrazones. The structures of the obtained compounds were elucidated by using IR, H-1-NMR and FAB(+)-MS spectral data and elemental analyses results. All of the compounds were screened for their antibacterial and antifungal activities against twelve different microorganisms by using microbroth dilution method. Ketoconazole and chloramphenicol were used as standard drugs. All of the compounds showed good activity against Staphylococcus aureus and Enterococcus faecalis.

WOS: 000320473000005, PubMed ID: 23681942, 1-(p-Methylphenyl)-3,5-diaryl-2-pyrazoline derivatives (2a-f) were synthesized via the treatment of 1-(1H-indol-3-yl)-3-aryl-2-propen-1-ones (1a-f) with p-methylphenylhydrazine hydrochloride in hot acetic acid. The structures of these compounds were elucidated by IR, 1H NMR, and mass spectral data and elemental analysis. These compounds were investigated for their antimicrobial activity. Brine-Shrimp lethality assay was carried out to determine the toxicity of the compounds. Compound 2e, which is the pyrazoline derivative bearing the 2,5-dichlorophenyl moiety, can be identified as the most promising agent against Klebsiella pneumoniae (ATCC 13883) and Candida glabrata (ATCC 36583) due to its inhibitory effects on K. pneumoniae and C. glabrata with a MIC value of 100 mu g/mL as a non-toxic agent (LC50>1000 mu g/mL).

WOS: 000295825600005, PubMed ID: 21975803, Due to antimicrobial importance of benzimidazoles and hydrazones, some benzimidazole-hydrazone compounds were synthesized to screen their antimicrobial activity. Structures of the synthesized compounds were elucidated by (1)H-NMR, IR and ES-MS spectral data and elemental analysis. The synthesized benzimidazole-hydrazones exhibited very weak antibacterial activity. However, antifungal activity of some of the synthesized compounds was very notable against Candida species. The compounds displaying important antifungal activity were screened for their toxicity. Artemia salina 96-well assay was used to determine cytotoxicity of the compounds. Tested compounds exhibited toxicity to different extents (LD(50) = 126.33-368.72 mu g/mL). Nevertheless, determination of 3-14 folds higher LD50 than minimum inhibitory concentration is a significant finding, which demonstrates that the compounds display antifungal activity at non-toxic concentration.

The biosorption of lead ions (Pb2+) onto lyophilized fungus Aspergillus niveus was investigated in aqueous solutions in a batch system with respect to pH, contact time and initial concentration of the ions at 30 °C. The maximum adsorption capacity of lyophilized A. niveus was found to be 92.6 mg g−1 at pH 5.1 and the biosorption equilibrium was established about in 30 min. The adsorption capacity obtained is one of the highest value among those reported in the literature. The kinetic data were analyzed using the pseudo-first-order kinetic, pseudo-second-order kinetic, and intraparticle diffusion equations. Kinetic parameters, such as rate constants, equilibrium adsorption capacities, and related correlation coefficients for the kinetic models were calculated and discussed. It was found that the adsorption of lead ions onto lyophilized A. niveus biomass fit the pseudo-second-order kinetic model well. The Langmuir and Freundlich isotherm parameters for the lead ion adsorption were applied and the Langmuir model agreed better with the adsorption of lead ions onto lyophilized A. niveus.

WOS: 000279521800005, PubMed ID: 20451306, In this study 12 novel benzimidazole compounds bearing hydrazone moiety were synthesized in order to investigate their possible antibacterial and antifungal activity. Structures of the synthesized compounds were elucidated by spectral data. Six different gram-negative and four different gram-positive bacterial strains were used in antibacterial activity tests. Antifungal activity tests were also performed against three different fungal strains. Most of the test compounds found to be significantly effective against Proteus vulgaris, Staphylococcus typhimurium, Klebsiella pneumoniae and Pseudomonas aeruginosa gram-negative bacterial strains. A structure activity relationship (SAR) study including some electronic parameters was carried out and a connection between antibacterial activity and electronic properties of the target compounds was determined. Toxicity of the most effective compounds was established by performing Brine Shrimp lethality assay

WOS: 000343236300008, In the present study, 5,5'-(1,4-phenylene)bis[3-(2-thienyl)-4,5-dihydro-1H-pyrazole-1-(4-arylthiazol-2-yl)] derivatives (3a-h) were obtained via the reaction of 5,5'-(1,4-phenylene)bis[3-(2-thienyl)-4,5-dihydro-1H-pyrazole-1-carbothioamide] (2) with phenacyl bromides. The synthesized compounds were investigated for their antimicrobial activity against various bacteria and Candida species. Among these derivatives, 5,5'-(1,4-phenylene)bis[3-(2-thienyl)-4,5-dihydro-1H-pyrazole-1-(4-(4-chlorophenyl)thiazol-2-yl)] (3b) and 5,5'-(1,4-phenylene)bis[3-(2-thienyl)-4,5-dihydro-1H-pyrazole- 1-(4-(4-methoxyphenyl) thiazol-2-yl)] (3d) showed notable antimicrobial activity.