Triazinoindole analogs as potent inhibitors of α-glucosidase: Synthesis, biological evaluation and molecular docking studies

• Published in: Bioorganic Chemistry
• Main Author: Rahim F.; Ullah K.; Ullah H.; Wadood A.; Taha M.; Rehman A.U.; Uddin I.; Ashraf M.; Shaukat A.; Rehman W.; Hussain S.; Khan K.M.
• Format: Article
• Language: English
• Published: Academic Press Inc. 2015
• Online Access: https://www.scopus.com/inward/record.uri?eid=2-s2.0-84919941245&doi=10.1016%2fj.bioorg.2014.12.001&partnerID=40&md5=79a338ff4fb9911bebc292bf68f10017
• ISSN: 452068
• DOI: 10.1016/j.bioorg.2014.12.001

A new series of triazinoindole analogs 1-11 were synthesized, characterized by EI-MS and 1H NMR, evaluated for α-glucosidase inhibitory potential. All eleven (11) analogs showed different range of α-glucosidase inhibitory potential with IC50 value ranging between 2.46 ± 0.008 and 312.79 ± 0.06 μM when compared with the standard acarbose (IC50, 38.25 ± 0.12 μM). Among the series, compounds 1, 3, 4, 5, 7, 8, and 11 showed excellent inhibitory potential with IC50 values 2.46 ± 0.008, 37.78 ± 0.05, 28.91 ± 0.0, 38.12 ± 0.04, 37.43 ± 0.03, 36.89 ± 0.06 and 37.11 ± 0.05 μM respectively. All other compounds also showed good enzyme inhibition. The binding modes of these analogs were confirmed through molecular docking. © 2014 Elsevier B.V. All rights reserved.