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Novel BK channel openers containing dehydroabietic acid skeleton: structure-activity relationship for peripheral substituents on ring C.

Bioorganic & medicinal chemistry letters (2008-09-16)
Yong-Mei Cui, Eriko Yasutomi, Yuko Otani, Takashi Yoshinaga, Katsutoshi Ido, Kohei Sawada, Tomohiko Ohwada
ABSTRACT

A series of dehydroabietic acid (DHAA, 2) derivatives was synthesized and evaluated as BK channel openers in an assay system of CHO-K1 cells expressing hBKalpha channels. Systematic modifications of the peripheral functionality of ring C of DHAA showed that the introduction of a nitro or (thio)urea group in ring C greatly enhanced the BK channel-opening activity.

MATERIALS
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Product Description

Sigma-Aldrich
Dehydroabietic acid, ≥95% (LC/MS-ELSD)