1.
Bioorg Med Chem
; 24(16): 3696-704, 2016 08 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-27312423
RESUMO
Thirty N-arylidenequinoline-3-carbohydrazides (1-30) have been synthesized and evaluated against ß-glucuronidase inhibitory potential. Twenty four analogs showed outstanding ß-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±1.25µM). Six analogs showed good ß-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 ß-glucuronidase inhibitors for further investigation.