Synthesis, Molecular Docking and Biological Properties of Novel Thiazolo[4,5-b]pyridine derivatives
2020
The synthesis, anti-inflammatory and antioxidant properties of novel 5-hydroxy-7-methyl-3 H -thiazolo[4,5- b ]pyridin-2-one derivatives were discussed. Fused thiazolo[4,5- b ]pyridin-2-ones were synthesized and modified at the N 3 , C 5 and C 6 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(2 H )-yl) propanenitrile ( 5 ) and thiazolo[4,5- b ]pyridin-3(2 H )-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.
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