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Choe YJ, Seo HN, Jung SY, Rhim H, Kim J, Choo DJ, Lee JY: Synthesis and SAR study of T-type calcium channel blockers. Arch Pharm. 2008 Oct;341(10):661-4.
Part II. . 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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