Abstract
Thirty N-arylidenequinoline-3-carbohydrazides (1-30) have been synthesized and evaluated against beta-glucuronidase inhibitory potential. Twenty four analogs showed outstanding b-glucuronidase activity having IC50 values ranging between 2.11 +/- 0.05 and 46.14 +/- 0.95 than standard D-saccharic acid 1,4 lactone (IC50 = 48.4 +/- 1.25 mu M). Six analogs showed good b-glucuronidase activity having IC50 values ranging between 49.38 +/- 0.90 and 80.10 +/- 1.80. Structure activity relationship and the interaction of the active compounds and enzyme active site with the help of docking studies were established. Our study identifies novel series of potent b-glucuronidase inhibitors for further investigation. (C) 2016 Elsevier Ltd. All rights reserved.