Synthesis, Molecular Docking and Biological Properties of Novel Thiazolo[4,5-b]pyridine derivatives
| Autor: | Taras I. Chaban, Julia E. Matiychuk, Olga Ya. Shyyka, Ihor G. Chaban, Volodymyr V. Ogurtsov, Ihor A. Nektegayev, Vasyl S. Matiychuk |
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| Jazyk: | angličtina |
| Rok vydání: | 2020 |
| Předmět: | |
| Zdroj: | Acta Chimica Slovenica, Vol 67, Iss 4, Pp 1035-1043 (2020) |
| Druh dokumentu: | article |
| ISSN: | 1318-0207 1580-3155 |
| DOI: | 10.17344/acsi.2019.5439 |
| Popis: | The synthesis, anti-inflammatory and antioxidant properties of novel 5-hydroxy-7-methyl-3H-thiazolo[4,5-b]pyridin-2-one derivatives were discussed. Fused thiazolo[4,5-b]pyridin-2-ones were synthesized and modified at the N3, C5 and C6 positions of the main core in order to obtain the compounds with a satisfactory pharmacological profile. The synthesized compounds were preselected via molecular docking for further testing of their anti-inflammatory activity in vitro. Evaluation of novel compounds over the carageenin induced rat paw edema revealed strong anti-inflammatory action of some compounds including (thiazolo[4,5-b]pyridin-3(2H)-yl) propanenitrile (5) and thiazolo[4,5-b]pyridin-3(2H)-yl) propanoic acid (6) even exceeding the standard – Ibuprofen. The antioxidant activity of the synthesized compounds was measured in vitro by the method of scavenging effect on 2,2-diphenyl-1-picrylhydrazyl (DPPH) radicals. |
| Databáze: | Directory of Open Access Journals |
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