Synthesis and SAR Study of T-Type Calcium Channel Blockers. Part II

Abstract

3,4-Dihydroquinazoline derivatives have been known to be the novel and potent T-type calcium channel blockers. From a systematic variation of 3,4-dihydroquinazoline derivative 5c (KYS05043), plausible SAR results were established. It was revealed that a 5-(dimethylamino)pentylamino group at R-1, a biphenyl group at R-2, and a benzyl amido group at R-3 in the 3,4-dihydroquinazoline backbone are closely related with the channel selectivity (T/N-type) as well as the potency based on the discovery of Q (KYS05090).