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

A new series of triazinoindole analogs 1-11 were synthesized, characterized by EI-MS and H-1 NMR, evaluated for alpha-glucosidase inhibitory potential. All eleven (11) analogs showed different range of alpha-glucosidase inhibitory potential with IC50 value ranging between 2.46 +/- 0.008 and 312.79 +/- 0.06 mu M when compared with the standard acarbose (IC50, 38.25 +/- 0.12 mu M). 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 mu M respectively. All other compounds also showed good enzyme inhibition. The binding modes of these analogs were confirmed through molecular docking. (C) 2014 Elsevier Inc. All rights reserved.