Abstract
alpha-Amylase is a target for type-2 diabetes mellitus treatment. However, small molecule inhibitors of alpha-amylase are currently scarce. In the course of developing small molecule alpha-amylase inhibitors, we designed and synthesized thiadiazole quinoline analogs (1-30), characterized by different spectroscopic techniques such as (HNMR)-H-1 and EI-MS and screened for alpha-amylase inhibitory potential. Thirteen analogs 1, 2, 3, 4, 5, 6, 22, 23, 25, 26, 27, 28 and 30 showed outstanding alpha-amylase inhibitory potential with IC50 values ranges between 0.002 +/- 0.60 and 42.31 +/- 0.17 lM which is many folds better than standard acarbose having IC50 value 53.02 +/- 0.12 mu M. Eleven analogs 7, 9, 10, 11, 12, 14, 15, 17, 18, 19 and 24 showed good to moderate inhibitory potential while seven analogs 8, 13, 16, 20, 21 and 29 were found inactive. Our study identifies novel series of potent alpha-amylase inhibitors for further investigation. Structure activity relationship has been established. (C) 2017 Elsevier Inc. All rights reserved.