DESIGN, SYNTHESIS, AND ANTIDIABETIC EVALUATION OF COUMARIN FUSED OXADIAZOLE DERIVATIVES

Abstract

Diabetes mellitus is a chronic metabolic disorder that leads to severe complications worldwide. In the present study, a series of new coumarin fused oxadiazole Schiff base derivatives (PM1-PM10) were synthesized by treating coumarin oxadiazole amines with different aromatic aldehydes. The structure of synthesized compounds was confirmed by IR, Mass, and 1H NMR. Further, these compounds were evaluated for ADME properties, molecular docking studies, and invitro α-glucosidase enzyme inhibition. The docking studies were performed with isomaltose from Saccharomyces cerevisiae (PDB Code 3A4A), with scores of -7.26 to -4.26 kcal/mol. Compound PM9 showed the best interaction among all these compounds having a ΔG of -7.26 kcal/mol compared with standard acarbose of - 6.85 kcal/mol. The glucosidase inhibitory activity showed IC50 31.10 to 21.33 μM and was compared with standard acarbose. Compound PM9 showed significant antidiabetic activity compared with the standard acarbose.