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Synthesis and SAR Study of T‐Type Calcium Channel Blockers. Part II
Author(s) -
Choe Yun Jeong,
Seo Han Na,
Jung Soo Yeon,
Rhim Hyewhon,
Kim Jungahn,
Choo Dong Joon,
Lee Jae Yeol
Publication year - 2008
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.200800079
Subject(s) - calcium channel , chemistry , potency , derivative (finance) , stereochemistry , selectivity , calcium , combinatorial chemistry , in vitro , biochemistry , organic chemistry , economics , financial economics , catalysis
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 ).