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10 results on '"Jampilek J"'

1. Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes-7.

Author

Gütschow M, Eynde JJV, Jampilek J, Kang C, Mangoni AA, Fossa P, Karaman R, Trabocchi A, Scott PJH, Reynisson J, Rapposelli S, Galdiero S, Winum JY, Brullo C, Prokai-Tatrai K, Sharma AK, Schapira M, Azuma YT, Cerchia L, Spetea M, Torri G, Collina S, Geronikaki A, García-Sosa AT, Vasconcelos MH, Sousa ME, Kosalec I, Tuccinardi T, Duarte IF, Salvador JAR, Bertinaria M, Pellecchia M, Amato J, Rastelli G, Gomes PAC, Guedes RC, Sabatier JM, Estévez-Braun A, Pagano B, Mangani S, Ragno R, Kokotos G, Brindisi M, González FV, Borges F, Miloso M, Rautio J, and Muñoz-Torrero D

Subjects
Animals, Chemistry, Pharmaceutical, Humans, Molecular Targeted Therapy, Pharmaceutical Preparations, Structure-Activity Relationship, Drug Discovery methods
Abstract

Breakthroughs in Medicinal Chemistry [...]., Competing Interests: The authors declare no conflict of interest.

Published
2020
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2. Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes-6.

Author

Vanden Eynde JJ, Mangoni AA, Rautio J, Leprince J, Azuma YT, García-Sosa AT, Hulme C, Jampilek J, Karaman R, Li W, Gomes PAC, Hadjipavlou-Litina D, Capasso R, Geronikaki A, Cerchia L, Sabatier JM, Ragno R, Tuccinardi T, Trabocchi A, Winum JY, Luque FJ, Prokai-Tatrai K, Spetea M, Gütschow M, Kosalec I, Guillou C, Vasconcelos MH, Kokotos G, Rastelli G, de Sousa ME, Manera C, Gemma S, Mangani S, Siciliano C, Galdiero S, Liu H, Scott PJH, de Los Ríos C, Agrofoglio LA, Collina S, Guedes RC, and Muñoz-Torrero D

Subjects
Humans, Chemistry, Pharmaceutical, Drug Discovery
Abstract

Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes is a series of Editorials that is published on a biannual basis by the Editorial Board of the Medicinal Chemistry section of the journal Molecules [...].

Published
2019
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3. Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes-5.

Author

Mangoni AA, Eynde JJV, Jampilek J, Hadjipavlou-Litina D, Liu H, Reynisson J, Sousa ME, Gomes PAC, Prokai-Tatrai K, Tuccinardi T, Sabatier JM, Luque FJ, Rautio J, Karaman R, Vasconcelos MH, Gemma S, Galdiero S, Hulme C, Collina S, Gütschow M, Kokotos G, Siciliano C, Capasso R, Agrofoglio LA, Ragno R, and Muñoz-Torrero D

Subjects
Humans, Chemistry, Pharmaceutical trends, Drug Discovery trends
Abstract

Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes is a series of Editorials which is published on a biannual basis by the Editorial Board of the Medicinal Chemistry section of the journal Molecules [...].

Published
2019
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4. Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes⁻4.

Author

Mangoni AA, Guillou C, Vanden Eynde JJ, Hulme C, Jampilek J, Li W, Prokai-Tatrai K, Rautio J, Collina S, Tuccinardi T, Sousa ME, Sabatier JM, Galdiero S, Karaman R, Kokotos G, Torri G, Luque FJ, Vasconcelos MH, Hadjipavlou-Litina D, Siciliano C, Gütschow M, Ragno R, Gomes PAC, Agrofoglio LA, and Muñoz-Torrero D

Subjects
Humans, Molecular Targeted Therapy, Drug Discovery methods
Abstract

Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes is a series of Editorials, which is published on a biannual basis by the Editorial Board of the Medicinal Chemistry section of the journal Molecules . [...]., Competing Interests: The authors declare no conflict of interest.

Published
2018
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5. Probability-driven 3D pharmacophore mapping of antimycobacterial potential of hybrid molecules combining phenylcarbamoyloxy and N-arylpiperazine fragments.

Author

Bak A, Kozik V, Malik I, Jampilek J, and Smolinski A

Subjects
Carbamates chemistry, Computer Simulation, In Vitro Techniques, Ligands, Probability, Anti-Bacterial Agents pharmacology, Drug Discovery, Models, Molecular, Mycobacterium tuberculosis drug effects, Quantitative Structure-Activity Relationship
Abstract

The current study examines in silico characterization of the structure-inhibitory potency for a set of phenylcarbamic acid derivatives containing an N-arylpiperazine scaffold, considering the electronic, steric and lipophilic properties. The main objective of the ligand-based modelling was the systematic study of classical comparative molecular field analysis (CoMFA)/comparative molecular surface analysis (CoMSA) performance for the modelling of in vitro efficiency observed for these phenylcarbamates, revealing their inhibitory activities against a virulent Mycobacterium tuberculosis H 37 R v strain. We compared the findings of efficiency modelling produced by a standard 3D methodology (CoMFA) and its neural counterparts (CoMSA) regarding multiple training/test subsets and variables used. Moreover, systematic space inspection, splitting values into the analysed training/test subsets, was performed to monitor statistical estimator performance while mapping the probability-driven pharmacophore pattern. Consequently, a 'pseudo-consensus' 3D-quantitative structure-activity relationship (3D-QSAR) approach was applied to retrieve an 'average' pharmacophore hypothesis by the investigation of the most densely populated training/test subpopulations to specify the potentially important factors contributing to the inhibitory activity of phenylcarbamic acid analogues. In addition, examination of descriptor-based similarity with a principal component analysis (PCA) procedure was employed to visualize noticeable variations in the performance of these molecules with respect to their structure and activity profiles.

Published
2018
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6. Design and Discovery of New Antibacterial Agents: Advances, Perspectives, Challenges.

Author

Jampilek J

Subjects
Animals, Anti-Bacterial Agents pharmacology, Cell Line, Drug Resistance, Bacterial drug effects, Gram-Negative Bacteria drug effects, Gram-Positive Bacteria drug effects, Humans, Anti-Bacterial Agents therapeutic use, Bacterial Infections drug therapy, Drug Design, Drug Discovery
Abstract

Background: Emerging resistance of bacterial pathogens to clinically used drugs, including not only first-choice but also second- and third-choice drugs, is alarming, but since the 1990s only a modest number of new, first in class, drugs for systemic administration have been marketed for the treatment of bacterial infections., Objective: This article provides a review of recently reported new antibacterial chemotherapeutics approved for clinical practice, antibacterial chemotherapeutics in clinical trials and antibacterial agents under development., Discussion: Antibacterial agents include new antibacterial compounds of used drug classes and new antibacterial agents with a novel mode of action. In addition, particular attention is given to agents decreasing bacterial resistance, i.e. to compounds that do not have significant intrinsic bacteriostatic or bactericidal activity, but in combination with antibacterial drugs are able to restore the effect of these drugs or demonstrate synergistic antibacterial properties together with the drugs., Conclusion: This review is specifically focused on small molecules rather than on peptides and discusses a wide range of various molecular scaffolds., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)

Published
2018
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7. How can we bolster the antifungal drug discovery pipeline?

Author

Jampilek J

Subjects
Antifungal Agents chemistry, Antifungal Agents pharmacology, Drug Design, Drug Resistance, Fungal drug effects, Echinocandins chemistry, Echinocandins pharmacology, Echinocandins therapeutic use, Glycosides chemistry, Glycosides pharmacology, Glycosides therapeutic use, Humans, Nanoparticles chemistry, Triterpenes chemistry, Triterpenes pharmacology, Triterpenes therapeutic use, Antifungal Agents therapeutic use, Drug Discovery, Mycoses drug therapy
Published
2016
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8. Potential of agricultural fungicides for antifungal drug discovery.

Author

Jampilek J

Subjects
Agrochemicals chemistry, Agrochemicals pharmacology, Animals, Antifungal Agents chemistry, Drug Design, Fungi drug effects, Fungicides, Industrial chemistry, Humans, Mycoses drug therapy, Structure-Activity Relationship, Antifungal Agents pharmacology, Drug Discovery methods, Fungicides, Industrial pharmacology
Abstract

While it is true that only a small fraction of fungal species are responsible for human mycoses, the increasing prevalence of fungal diseases has highlighted an urgent need to develop new antifungal drugs, especially for systemic administration. This contribution focuses on the similarities between agricultural fungicides and drugs. Inorganic, organometallic and organic compounds can be found amongst agricultural fungicides. Furthermore, fungicides are designed and developed in a similar fashion to drugs based on similar rules and guidelines, with fungicides also having to meet similar criteria of lead-likeness and/or drug-likeness. Modern approved specific-target fungicides are well-characterized entities with a proposed structure-activity relationships hypothesis and a defined mode of action. Extensive toxicological evaluation, including mammalian toxicology assays, is performed during the whole discovery and development process. Thus modern agrochemical research (design of modern agrochemicals) comes close to drug design, discovery and development. Therefore, modern specific-target fungicides represent excellent lead-like structures/models for novel drug design and development.

Published
2016
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9. Breakthroughs in medicinal chemistry: new targets and mechanisms, new drugs, new hopes-7

Author

Gütschow, Michael, Eynde, Jean Jacques Vanden, Jampilek, Josef, Kang, CongBao, Mangoni, Arduino, Fossa, Paola, Karaman, Rafik, Trabocchi, Andrea, Scott, Peter, Reynisson, Jóhannes, Rapposelli, Simona, Galdiero, Stefania, Winum, Jean-Yves, Brullo, Chiara, Prokai-Tatrai, Katalin, Sharma, Arun, Schapira, Matthieu, Azuma, Yasu-Taka, Cerchia, Laura, Spetea, Mariana, Torri, Giangiacomo, Collina, Simona, Geronikaki, Athina, García-Sosa, Alfonso, Vasconcelos, M Helena, Sousa, Maria Emília, Kosalec, Ivan, Tuccinardi, Tiziano, Duarte, Iola, Salvador, Jorge, Bertinaria, Massimo, Pellecchia, Maurizio, Amato, Jussara, Rastelli, Giulio, Gomes, Paula, Guedes, Rita, Sabatier, Jean-Marc, Estévez-Braun, Ana, Pagano, Bruno, Mangani, Stefano, Ragno, Rino, Kokotos, George, Brindisi, Margherita, González, Florenci, Borges, Fernanda, Miloso, Mariarosaria, Rautio, Jarkko, Muñoz-Torrero, Diego, Vanden Eynde, Jean Jacques, Vasconcelos, M. Helena, Gutschow, M., Eynde, J. J. V., Jampilek, J., Kang, C., Mangoni, A. A., Fossa, P., Karaman, R., Trabocchi, A., Scott, P. J. H., Reynisson, J., Rapposelli, S., Galdiero, S., Winum, J. -Y., Brullo, C., Prokai-Tatrai, K., Sharma, A. K., Schapira, M., Azuma, Y. -T., Cerchia, L., Spete, M., Torri, G., Collina, S., Geronikaki, A., Garcia-Sosa, A. T., Helena Vasconcelos, M., Sousa, M. E., Kosalec, I., Tuccinardi, T., Duarte, I. F., Salvador, J. A. R., Bertinaria, M., Pellecchia, M., Amato, J., Rastelli, G., Gomes, P. A. C., Guedes, R. C., Sabatier, J. -M., Estevez-Braun, A., Pagano, B., Mangani, S., Ragno, R., Kokotos, G., Brindisi, M., Gonzalez, F. V., Borges, F., Miloso, M., Rautio, J., Munoz-Torrero, D., Institut de neurophysiopathologie (INP), Aix Marseille Université (AMU)-Centre National de la Recherche Scientifique (CNRS), Gutschow, M, Eynde, J, Jampilek, J, Kang, C, Mangoni, A, Fossa, P, Karaman, R, Trabocchi, A, Scott, P, Reynisson, J, Rapposelli, S, Galdier, S, Winum, J, Brullo, C, Prokai-Tatrai, K, Sharma, A, Schapira, M, Azuma, Y, Cerchia, L, Spete, M, Torri, G, Collina, S, Geronikaki, A, Garcia-Sosa, A, Helena Vasconcelos, M, Sousa, M, Kosalec, I, Tuccinardi, T, Duarte, I, Salvador, J, Bertinaria, M, Pellecchia, M, Amato, J, Rastelli, G, Gomes, P, Guedes, R, Sabatier, J, Estevez-Braun, A, Pagano, B, Mangani, S, Ragno, R, Kokotos, G, Brindisi, M, Gonzalez, F, Borges, F, Miloso, M, Rautio, J, and Munoz-Torrero, D

Subjects
RM, Pharmaceutical research, molecular targeted therapy, Chemistry, Pharmaceutical, MESH: Pharmaceutical Preparations, [SDV]Life Sciences [q-bio], Pharmaceutical Science, animals, chemistry, pharmaceutical, drug discovery, humans, pharmaceutical preparations, structure-activity relationship, Q1, chemistry, 01 natural sciences, Clinical chemistry, Analytical Chemistry, lcsh:QD241-441, 03 medical and health sciences, MESH: Chemistry, Pharmaceutical, Química clínica, MESH: Structure-Activity Relationship, lcsh:Organic chemistry, MESH: Drug Discovery, CHIM/06 - CHIMICA ORGANICA, MESH: Molecular Targeted Therapy, pharmaceutical, MESH: Animals, RM695, Investigació farmacèutica, Physical and Theoretical Chemistry, 030304 developmental biology, 0303 health sciences, MESH: Humans, 010405 organic chemistry, Medicinal Chemistry, New Targets, New Mechanisms, New Drugs, Organic Chemistry, R735, R1, 3. Good health, 0104 chemical sciences, Editorial, n/a, Chemistry (miscellaneous), Molecular Medicine, Breakthroughs, Medicinal Chemistry, medicinal chemistry, targets, drugs, molecules, [SDV.MHEP]Life Sciences [q-bio]/Human health and pathology
Abstract

Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes is a series of editorials which is published on a biannual basis by the Editorial Board of the Medicinal Chemistry section of the journal Molecules. In these editorials, we highlight in brief reports (of about one hundred words) a number of recently published articles that describe crucial findings, such as the discovery of novel drug targets and mechanisms of action or novel classes of drugs, which may inspire future medicinal chemistry endeavors devoted to addressing prime unmet medical needs.

Published
2020

10. Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes–5

Author

Arduino Mangoni, Jean Eynde, Josef Jampilek, Dimitra Hadjipavlou-Litina, Hong Liu, Jóhannes Reynisson, Maria Sousa, Paula Gomes, Katalin Prokai-Tatrai, Tiziano Tuccinardi, Jean-Marc Sabatier, F. Luque, Jarkko Rautio, Rafik Karaman, M. Vasconcelos, Sandra Gemma, Stefania Galdiero, Christopher Hulme, Simona Collina, Michael Gütschow, George Kokotos, Carlo Siciliano, Raffaele Capasso, Luigi Agrofoglio, Rino Ragno, Diego Muñoz-Torrero, Flinders University [Adelaide, Australia], University of Mons [Belgium] (UMONS), Comenius University in Bratislava, Aristotle University of Thessaloniki, Chinese Academy of Sciences [Beijing] (CAS), Keele University [Keele], Universidade do Porto, University of North Texas Health Science Center [Fort Worth], University of Pisa - Università di Pisa, Institut de neurophysiopathologie (INP), Aix Marseille Université (AMU)-Centre National de la Recherche Scientifique (CNRS), University of Barcelona, University of Eastern Finland, Al-Quds University, University of Siena (University of Siena), University of Naples Federico II, University of Arizona, University of Pavia, University of Bonn, National and Kapodistrian University of Athens (NKUA), University of Calabria, Institut de Chimie Organique et Analytique (ICOA), Université d'Orléans (UO)-Centre National de la Recherche Scientifique (CNRS)-Commissariat à l'énergie atomique et aux énergies alternatives (CEA)-Institut de Chimie du CNRS (INC)-Institut National de la Santé et de la Recherche Médicale (INSERM), Università degli Studi di Roma 'La Sapienza' = Sapienza University [Rome], Universitat de Barcelona, Universidade do Porto = University of Porto, Università degli Studi di Siena = University of Siena (UNISI), University of Naples Federico II = Università degli studi di Napoli Federico II, Università degli Studi di Pavia = University of Pavia (UNIPV), Universität Bonn = University of Bonn, Università della Calabria [Arcavacata di Rende] (Unical), Commissariat à l'énergie atomique et aux énergies alternatives (CEA)-Université d'Orléans (UO)-Institut National de la Santé et de la Recherche Médicale (INSERM)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS), Università degli Studi di Roma 'La Sapienza' = Sapienza University [Rome] (UNIROMA), Instituto de Investigação e Inovação em Saúde, Leloup, Ludovic, Mangoni, A. A., Eynde, J. J. V., Jampilek, J., Hadjipavlou-Litina, D., Liu, H., Reynisson, J., Sousa, M. E., Gomes, P. A. C., Prokai-Tatrai, K., Tuccinardi, T., Sabatier, J. -M., Luque, F. J., Rautio, J., Karaman, R., Vasconcelos, M. H., Gemma, S., Galdiero, S., Hulme, C., Collina, S., Gutschow, M., Kokotos, G., Siciliano, C., Capasso, Raffaele, Agrofoglio, L. A., Ragno, R., and Munoz-Torrero, D.

Subjects
Chemistry, Pharmaceutical, [SDV]Life Sciences [q-bio], Pharmaceutical Science, Drug Discovery / trends, Química farmacèutica, 010402 general chemistry, 01 natural sciences, Analytical Chemistry, RS, lcsh:QD241-441, 03 medical and health sciences, lcsh:Organic chemistry, Drug Discovery, [CHIM] Chemical Sciences, Humans, [CHIM]Chemical Sciences, Physical and Theoretical Chemistry, ComputingMilieux_MISCELLANEOUS, 030304 developmental biology, breakthroughs in medicinal chemistry, new targets, new mechanisms, new drugs, 0303 health sciences, [SDV.MHEP] Life Sciences [q-bio]/Human health and pathology, Organic Chemistry, 3. Good health, 0104 chemical sciences, [SDV] Life Sciences [q-bio], Chemistry, Editorial, Chemistry, Pharmaceutical / trends, n/a, Chemistry (miscellaneous), Pharmaceutical, Molecular Medicine, Pharmaceutical chemistry, [SDV.MHEP]Life Sciences [q-bio]/Human health and pathology
Abstract

Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes is a series of Editorials which is published on a biannual basis by the Editorial Board of the Medicinal Chemistry section of the journal Molecules. In these Editorials, we highlight in brief reports (of about one hundred words) a number of recently published articles that describe crucial findings, such as the discovery of novel drug targets and mechanisms of action or novel classes of drugs, which may inspire future medicinal chemistry endeavors devoted to addressing prime unmet medical needs.

Published
2019

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