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Article

Synthesis and Biological Activity Evaluation of Novel 5-Methyl-7-Phenyl-3H-Thiazolo[4,5-b]Pyridin-2-Ones

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Department of Pharmaceutical, Organic and Bioorganic Chemistry, Danylo Halytsky Lviv National Medical University, 69 Pekarska, 79010 Lviv, Ukraine
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Department of Microbiology, Danylo Halytsky Lviv National Medical University, 69 Pekarska, 79010 Lviv, Ukraine
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Institute of Cell Biology, NAS of Ukraine, 14/16 Drahomanova, 79005 Lviv, Ukraine
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Department of Organic Chemistry, Medical University of Lublin, Aleje Racławickie 1, 20-059 Lublin, Poland
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Enamine Ltd., 23 Alexandra Matrosova, 01103 Kyiv, Ukraine
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Department of Pharmaceutical Chemistry, National Pirogov Memorial Medical University, 56 Pirogov, 21018 Vinnytsya, Ukraine
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Department of Biotechnology and Cell Biology, Medical College, University of Information Technology and Management in Rzeszow, Sucharskiego 2, 35-225 Rzeszow, Poland
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Author to whom correspondence should be addressed.
Academic Editor: Thierry Besson
Sci. Pharm. 2021, 89(4), 52; https://doi.org/10.3390/scipharm89040052 (registering DOI)
Received: 26 October 2021 / Revised: 20 November 2021 / Accepted: 23 November 2021 / Published: 25 November 2021
(This article belongs to the Special Issue Heterocyclic Chemistry in Drug Design 2.0)
A series of 5-methyl-7-phenyl-3H-thiazolo[4,5-b]pyridin-2-ones has been designed, synthesized, and characterized by spectral data. Target compounds were screened for their antimicrobial activity against some pathogenic bacteria and fungi, and most of them showed moderate activity, especially compound 3g, which displayed the potent inhibitory effect against Pseudomonas aeruginosa and Escherichia coli with MIC value of 0.21 μM. The active thiazolopyridine derivatives 3c, 3f, and 3g were screened for their cytotoxicity effects on HaCat, Balb/c 3T3 cells using MTT assay, which revealed promising results. In silico assessment for compounds 3c, 3f, and 3g also revealed suitable drug-like parameters and ADME properties. The binding interactions of the most active compound 3g were performed through molecular docking against MurD and DNA gyrase, with binding energies and an inhibitory constant compared to the reference drug ciprofloxacin. The tested thiazolo[4,5-b]pyridines constitute an exciting background for the further development of new synthetic antimicrobial agents. View Full-Text
Keywords: thiazolo[4,5-b]pyridines; antimicrobial activity; pharmacokinetics prediction; molecular docking thiazolo[4,5-b]pyridines; antimicrobial activity; pharmacokinetics prediction; molecular docking
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MDPI and ACS Style

Lozynskyi, A.; Konechnyi, Y.; Senkiv, J.; Yushyn, I.; Khyluk, D.; Karpenko, O.; Shepeta, Y.; Lesyk, R. Synthesis and Biological Activity Evaluation of Novel 5-Methyl-7-Phenyl-3H-Thiazolo[4,5-b]Pyridin-2-Ones. Sci. Pharm. 2021, 89, 52. https://doi.org/10.3390/scipharm89040052

AMA Style

Lozynskyi A, Konechnyi Y, Senkiv J, Yushyn I, Khyluk D, Karpenko O, Shepeta Y, Lesyk R. Synthesis and Biological Activity Evaluation of Novel 5-Methyl-7-Phenyl-3H-Thiazolo[4,5-b]Pyridin-2-Ones. Scientia Pharmaceutica. 2021; 89(4):52. https://doi.org/10.3390/scipharm89040052

Chicago/Turabian Style

Lozynskyi, Andrii, Yulian Konechnyi, Julia Senkiv, Ihor Yushyn, Dmytro Khyluk, Olexandr Karpenko, Yulia Shepeta, and Roman Lesyk. 2021. "Synthesis and Biological Activity Evaluation of Novel 5-Methyl-7-Phenyl-3H-Thiazolo[4,5-b]Pyridin-2-Ones" Scientia Pharmaceutica 89, no. 4: 52. https://doi.org/10.3390/scipharm89040052

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