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Bioorg Med Chem Lett. 2008 Oct 1;18(19):5201-5. doi: 10.1016/j.bmcl.2008.08.078. Epub 2008 Aug 28.

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

Author information

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

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.

PMID:
18789860
DOI:
10.1016/j.bmcl.2008.08.078
[Indexed for MEDLINE]

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