Discovery and evaluation of selective N-type calcium channel blockers: 6-Unsubstituted-1,4-dihydropyridine-5-carboxylic acid derivatives
- 作者：Takashi Yamamoto ; takashia_yamamoto@ajinomoto.com ; Seiji Niwa ; Munetaka Tokumasu ; Tomoyuki Onishi ; Seiji Ohno ; Masako Hagihara ; Hajime Koganei ; Shin-ichi Fujita ; Tomoko Takeda ; Yuki Saitou ; Satoshi Iwayama ; Akira Takahara ; Seinosuke Iwata ; Masataka Shoji
- 关键词：N-Type calcium channel blocker ; Structure&ndash ; activity relationships ; 1 ; 4-Dihydropyridine derivative
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2012
- 期刊代码：10_0960894x
- 类别：ch
- 出版时间：1 June, 2012
- 卷：22
- 期：11
- 页码：3639-3642
- 文件大小：388 K
摘要
A structure-activity relationship study of 6-unsubstituted-1,4-dihydropyridine and 2,6-unsubstituted-1,4-dihydropyridine derivatives was conducted in an attempt to discover N-type calcium channel blockers that were highly selective over L-type calcium channel blockers. Among the tested compounds, (+)-4-(3,5-dichloro-4-methoxy-phenyl)-1,4-dihydro-pyridine-3,5-dicarboxylic acid 3-cinnamyl ester was found to be an effective and selective N-type calcium channel blocker with oral analgesic potential.