Synthesis and SAR study of T-type calcium channel blockers. 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).
Choe
Yun Jeong
YJ
Research Institute for Basic Sciences and Department of Chemistry, College of Sciences, Kyung Hee University, Seoul, Korea.
Seo
Han Na
HN
Jung
Soo Yeon
SY
Rhim
Hyewhon
H
Kim
Jungahn
J
Choo
Dong Joon
DJ
Lee
Jae Yeol
JY
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
D002121:Calcium Channel Blockers; D020747:Calcium Channels, T-Type; D011799:Quinazolines