The synthesis and BK channel-opening activity of N-acylaminoalkyloxime derivatives of dehydroabietic acid
The synthesis and BK channel-opening activity of N-acylaminoalkyloxime derivatives of dehydroabietic acid
复制标题
脱氢松香酸N-酰氨基烷基肟衍生物的合成及其BK通道开放活性。
DOI：
10.1016/j.bmcl.2015.12.038
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发表时间：
2016-01-15
影响因子：
2.7
通讯作者：
Sawada, Kohei
中科院分区：
文献类型：
--
作者：
Cui, Yong-Mei;Liu, Xin-Lan;Sawada, Kohei
合成了一系列脱氢松香酸的N-酰基氨基烷基肟衍生物，并在表达hBK α通道的CHO-K1细胞的测定系统中评价了BK通道开放活性。构效关系研究表明，2-噻吩的S原子与羰基O原子之间存在非共价相互作用，这可能是其与离子通道相互作用的构象限制。该研究对松香烷类BK通道开放剂的设计和合成具有指导意义。(C)2015爱思唯尔有限公司版权所有。
A series of N-acylaminoalkyloxime derivatives of dehydroabietic acid were synthesized and evaluated for BK channel-opening activities in an assay system of CHO-K1 cells expressing hBK alpha channels. The structure-activity relationship study revealed that a non-covalent interaction between the S atom of the 2-thiophene and the carbonyl O atom may contribute to conformation restriction for interaction with the ion channel. This research could guide the design and synthesis of novel abietane-based BK channel opener. (C) 2015 Elsevier Ltd. All rights reserved.