期刊
MOLECULAR DIVERSITY
卷 25, 期 4, 页码 2399-2409出版社
SPRINGER
DOI: 10.1007/s11030-020-10137-8
关键词
Carbamates; alpha-Glucosidase; 4-Alkylaminoimidazo[1,2-a]pyridine; Synthesis
类别
资金
- Tehran University of Medical Sciences [98-03-33-43696]
A series of imidazo[1,2-a]pyridines linked to carbamate moiety were designed, synthesized, and evaluated for their alpha-glucosidase inhibitory activity. Compound 6d exhibited the most potent inhibition with a competitive mechanism, as supported by kinetic and molecular docking studies. Hydrogen bonds and electrostatic interactions in the active site contributed to the well-oriented conformation of compound 6d.
In this work, various imidazo[1,2-a]pyridines linked to carbamate moiety were designed, synthesized, and evaluated for their alpha-glucosidase inhibitory activity. Among synthesized compounds, 4-(3-(tert-Butylamino)imidazo[1,2-a]pyridin-2-yl)phenylp-tolylcarbamate (6d) was the most potent compound (IC50 = 75.6 mu M) compared with acarbose as the reference drug (IC50 = 750.0 mu M). Kinetic study of compound6dindicated a competitive inhibition. Also, the molecular docking study suggested desired interactions with the active site residues. In particular, hydrogen bonds and electrostatic interactions constructed by compound 6d afforded well-oriented conformation in the 3A4A active site.
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