| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1366982 | Bioorganic & Medicinal Chemistry Letters | 2007 | 5 Pages |
Abstract
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).
Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Ja Youn Choi, Han Na Seo, Min Joo Lee, Seong Jun Park, Sung Jun Park, Ji Young Jeon, Joo Hi Kang, Ae Nim Pae, Hyewhon Rhim, Jae Yeol Lee,
