Evaluation and docking of indole sulfonamide as a potent inhibitor of α-glucosidase enzyme in streptozotocin –induced diabetic albino wistar rats

• Published in: Bioorganic Chemistry
• Main Author: Taha M.; Imran S.; Salahuddin M.; Iqbal N.; Rahim F.; Uddin N.; Shehzad A.; Khalid Farooq R.; Alomari M.; Mohammed Khan K.
• Format: Article
• Language: English
• Published: Academic Press Inc. 2021
• Online Access: https://www.scopus.com/inward/record.uri?eid=2-s2.0-85102849446&doi=10.1016%2fj.bioorg.2021.104808&partnerID=40&md5=3378c9754bd5cd1f09b1097f773a98af

We have synthesized new hybrid class of indole bearing sulfonamide scaffolds (1–17) as α-glucosidase inhibitors. All scaffolds were found to be active except scaffold 17 and exhibited IC50 values ranging from 1.60 to 51.20 µM in comparison with standard acarbose (IC50 = 42.45 µM). Among the synthesized hybrid class scaffolds 16 was the most potent analogue with IC50 value 1.60 μM, showing many folds better potency as compared to standard acarbose. Whereas, synthesized scaffolds 1–15 showed good α-glucosidase inhibitory potential. Based on α-glucosidase inhibitory effect, Scaffold 16 was chosen due to highest activity in vitro for further evaluation of antidiabetic activity in Streptozotocin induced diabetic rats. The Scaffold 16 exhibited significant antidiabetic activity. All analogues were characterized through 1H, 13CNMR and HR MS. Structure-activity relationship of synthesized analogues was established and confirmed through molecular docking study. © 2021 Elsevier Inc.