Synthesis of multiple biologically active 1, 2-dihydro-pyrimido [1, 2-A]-benzimidazole-3- carbonitrile.

ABSTRACT

A variety of 1,2-dihydropyrimido-[1,2-a]-benzimidazole-3-carbonitrile derivatives were synthesized under microwave irradiation using water and acetonitril as solvent system. All the compounds were tested in vitro for α-glucosidase inhibitory and DPPH free radical scavenging activity. 4-Amino-2-(4-flourophenyl)-1,2-dihydropyrimido [1,2-a]-benzimidazole-3-carbonitrile (4c) was found to be a potent intestinal α- glucosidase inhibi tory activity (IC50; 91μM) along with moderate DPPH scavenging property. This compound was further evaluated for cytotoxicity activity against HT-29 colon cancer cell line. The IC50 value for its cytotoxicity activity was found to be 662 μM.