title: 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 6k (KYS05090).
authors.affiliation: Research Institute for Basic Sciences and Department of Chemistry, College of Sciences, Kyung Hee University, Seoul, Korea.
authors.forename: Yun Jeong
authors.initials: YJ
authors.lastname: Choe
authors.forename: Han Na
authors.initials: HN
authors.lastname: Seo
authors.forename: Soo Yeon
authors.initials: SY
authors.lastname: Jung
authors.forename: Hyewhon
authors.initials: H
authors.lastname: Rhim
authors.forename: Jungahn
authors.initials: J
authors.lastname: Kim
authors.forename: Dong Joon
authors.initials: DJ
authors.lastname: Choo
authors.forename: Jae Yeol
authors.initials: JY
authors.lastname: Lee
mesh_terms: D002121:Calcium Channel Blockers / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D020747:Calcium Channels, T-Type / Q000378:metabolism*; D002460:Cell Line; D015195:Drug Design; D006801:Humans; D015394:Molecular Structure; D011799:Quinazolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D002121:Calcium Channel Blockers; D020747:Calcium Channels, T-Type; D011799:Quinazolines