| Autor: |
Chaban TI, Matiichuk YE, Shyyka OY, Chaban IG, Ogurtsov VV, Nektegayev IA, Matiychuk VS |
| Jazyk: |
angličtina |
| Zdroj: |
Acta chimica Slovenica [Acta Chim Slov] 2020 Dec; Vol. 67 (4), pp. 1035-1043. |
| Abstrakt: |
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: |
MEDLINE |
| Externí odkaz: |
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