Abstract
A series consisting of 1–25 5-indole hydrazone have been synthesized and evaluated for their alpha amylase inhibition.
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•Synthesis of indole derivatives.•In vitro alpha amylase activity.•Identification of a new class of alpha amylase inhibitor.•Structure Activity Relationship established.•Molecular docking.
Twenty five derivatives of indole carbohydrazide (1–25) had been synthesized. These compounds were characterized using 1H NMR and EI-MS, and further evaluated for their α-amylase inhibitory potential. The analogs (1–25) showed varying degree of α-amylase inhibitory potential.
ranging between 9.28 and 599.0µM when compared with standard acarbose having IC50 value 8.78±0.16µM. Six analogs, 25 (IC50=9.28±0.153µM), 22 (IC50=9.79±0.43µM), 4 (IC50=11.08±0.357µM), 1 (IC50=12.65±0.169µM), 8 (IC50=21.37±0.07µM) and 14 (IC50=43.21±0.14µM) showed potent α-amylase inhibition as compared to the standard acarbose (IC50=8.78±0.16µM). All other analogs displayed good to moderate inhibitory potential. Structure-activity relationship was established through the interaction of the active compounds with enzyme active site with the help of docking studies.