Novel BK channel openers containing dehydroabietic acid skeleton: structure-activity relationship for peripheral substituents on ring C.
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.
Cui
Yong-Mei
YM
Graduate School of Pharmaceutical Sciences, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-0033, Japan.
Yasutomi
Eriko
E
Otani
Yuko
Y
Yoshinaga
Takashi
T
Ido
Katsutoshi
K
Sawada
Kohei
K
Ohwada
Tomohiko
T
D045784:Abietanes / Q000737:chemistry* / Q000494:pharmacology*; D000818:Animals; D002264:Carboxylic Acids / Q000737:chemistry*; D020650:Combinatorial Chemistry Techniques; D006224:Cricetinae; D003412:Cricetulus; D015640:Ion Channel Gating / Q000187:drug effects*; D051036:Large-Conductance Calcium-Activated Potassium Channels / Q000187:drug effects*; D008958:Models, Molecular; D015394:Molecular Structure; D018408:Patch-Clamp Techniques; D013329:Structure-Activity Relationship
D045784:Abietanes; D002264:Carboxylic Acids; D051036:Large-Conductance Calcium-Activated Potassium Channels; C013913:dehydroabietic acid