2. Academic Validation
  3. The structure-activity relationship study on 2-, 5-, and 6-position of the water soluble 1,4-dihydropyridine derivatives blocking N-type calcium channels

The structure-activity relationship study on 2-, 5-, and 6-position of the water soluble 1,4-dihydropyridine derivatives blocking N-type calcium channels

  • Bioorg Med Chem Lett. 2008 Sep 1;18(17):4813-6. doi: 10.1016/j.bmcl.2008.07.096.
Takashi Yamamoto 1,  Seiji Niwa,  Seiji Ohno,  Munetaka Tokumasu,  Yoko Masuzawa,  Chika Nakanishi,  Akira Nakajo,  Tomoyuki Onishi,  Hajime Koganei,  Shin-Ichi Fujita,  Tomoko Takeda,  Morikazu Kito,  Yukitsugu Ono,  Yuki Saitou,  Akira Takahara,  Seinosuke Iwata,  Masataka Shoji
Affiliations

Affiliation

  • 1 Pharmaceutical Research Laboratory, Ajinomoto company Inc., 1-1, Suzuki-cho, Kawasaki-ku, Kawasaki-shi, Japan.
PMID: 18684623 DOI: 10.1016/j.bmcl.2008.07.096
Abstract

In order to find an injectable and selective N-type calcium channel blocker, we have performed the structure-activity relationship (SAR) study on the 2-, 5-, and 6-position of 1,4-dihydropyridine-3-carboxylate derivative APJ2708 (2), which is a derivative of Cilnidipine and has L/N-type calcium channel dual inhibitory activities. As a consequence of the optimization, 6-dimethylacetal derivative 7 was found to have an effective inhibitory activity against N-type calcium channels with more than 170-fold lower activity for L-type channel compared to that of APJ2708.

Figures
嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z