928006-46-6Relevant academic research and scientific papers
Synthesis and SAR study of T-type calcium channel blockers. Part II
Yun, Jeong Choe,Han, Na Seo,Soo, Yeon Jung,Rhim, Hyewhon,Kim, Jungahn,Dong, Joon Choo,Jae, Yeol Lee
experimental part, p. 661 - 664 (2009/04/07)
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 R2, and a benzyl amido group at R3 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).
Synthesis and biological evaluation of novel T-type calcium channel blockers
Choi, Ja Youn,Seo, Han Na,Lee, Min Joo,Park, Seong Jun,Park, Sung Jun,Jeon, Ji Young,Kang, Joo Hi,Pae, Ae Nim,Rhim, Hyewhon,Lee, Jae Yeol
, p. 471 - 475 (2007/10/03)
3,4-Dihydroquinazoline analogues substituted by N-methyl-N-(5-pyrrolidinopentyl)amine at the 2-position were synthesized and their blocking effects were evaluated for T- and N-type calcium channels. Compound 11b (KYS05080), compared to mibefradil (IC50 = 1.34 ± 0.49 μM), was about 5-fold potent (IC50 = 0.26 ± 0.01 μM) for T-type calcium channel (α1G) blocking and its selectivity of T/N-type was also improved (7.5 versus 1.4 of mibefradil).
