SYNTHESIS, DOCKING STUDIES AND BIOLOGICAL EVALUATION OF SOME NEWLY SUBSTITUTED-5-(2 - METHYL IMIDAZO [1, 2-a] PYRIDIN-3 -YL) -2, 5 - DIHYDRO -1, 3, 4 -THIADIAZOL-2-AMINES

摘要

Objective: To synthesize and study the docking pattern and Anti inflammatory activities of some new analogues of Imidazo [1, 2-a] pyridines. Methods: A scheme involving the synthesis of a modern series of ten substituted 5-(2-Methyl imidazo [1, 2-a] pyridine-3- yl) -2, 5 -dihydro -1, 3, 4- thiadiazol-2-amines (6a- j) using 2-amino pyridine 1 as the starting material, through an order of four reactions was proposed. The derivatives were subjected to docking studies using the protein sequences for prostaglandin reductase. It was found that all the synthesized derivatives possessed very good binding energy, bringing into consideration that, the compounds are good inhibitors of prostaglandin reductase and hence are vested with anti-inflammatory properties. The scheme was then practically preceded and the synthesized compounds were characterized based on spectral data and elemental analysis. The new moieties were then evaluated for invitro anti-inflammatory property by Human Red Blood cell (HRBC) membrane stabilization method using Diclofenac as the standard drug. Results: All the compounds synthesized showed inhibition of inflammation out of which compounds 6a, 6b, 6c & 6f possessing meta nitro, para nitro, meta hydroxy and trimethoxy substitution respectively were identified as significant inhibitors of inflammation when compared with the activity of standard drug Diclofenac. Conclusion: On comparing the docking scores of the compounds with their anti-inflammatory activity, it is evident that derivatives 6b, 6d and 6f that showed excellent docking scores, possessed maximum anti-inflammatory property