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12,14-二氯脱氢枞酸的新型肟和肟醚衍生物:设计、合成及BK通道开放活性

Novel oxime and oxime ether derivatives of 12,14-dichlorodehydroabietic acid: design, synthesis, and BK channel-opening activity.

作者信息

Cui Yong-Mei, Yasutomi Eriko, Otani Yuko, Yoshinaga Takashi, Ido Katsutoshi, Sawada Kohei, Kawahata Masatoshi, Yamaguchi Kentaro, Ohwada Tomohiko

机构信息

Graduate School of Pharmaceutical Sciences, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-0033, Japan.

出版信息

Bioorg Med Chem Lett. 2008 Dec 15;18(24):6386-9. doi: 10.1016/j.bmcl.2008.10.078. Epub 2008 Oct 22.

Abstract

Oxime ether derivatives of the benzylic ketone of 12,14-dichlorodehydroabietic acid (diCl-DHAA, 4b) were synthesised, and their BK channel-opening activity was evaluated in an assay system of CHO-K1 cells expressing hBKalpha channels. Oxime ether structure on the B ring of diCl-DHAA significantly increased the BK channel-opening activity.

摘要

合成了12,14-二氯脱氢枞酸(diCl-DHAA,4b)苄基酮的肟醚衍生物,并在表达hBKα通道的CHO-K1细胞检测系统中评估了它们的BK通道开放活性。diCl-DHAA B环上的肟醚结构显著提高了BK通道开放活性。

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