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Synthesis and SAR study of T-type calcium channel blockers. Part II
Yun Jeong Choe1, Han Na Seo, Soo Yeon Jung
1Research Institute for Basic Sciences and Department of Chemistry, College of Sciences, Kyung Hee University, Seoul, Korea.
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 6k (KYS05090).
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