The discovery of a new class of large-conductance Ca2+-activated K+ channel opener targeted for overactive bladder:: Synthesis and structure-activity relationships of 2-amino-4-azaindoles

被引：21

作者：

Turner, SC ^{[1
]}

Carroll, WA ^{[1
]}

White, TK ^{[1
]}

Gopalakrishnan, M ^{[1
]}

Coghlan, MJ ^{[1
]}

Shieh, CC ^{[1
]}

Zhang, XF ^{[1
]}

Parihar, AS ^{[1
]}

Buckner, SA ^{[1
]}

Milicic, I ^{[1
]}

Sullivan, JP ^{[1
]}

机构：

[1] Abbott Labs, Global Pharmaceut Res & Dev, Neurosci Res, Abbott Pk, IL 60064 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 12期

关键词：

D O I：

10.1016/S0960-894X(03)00324-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

2-Amino-4-azaindoles have been identified as a structurally novel class of BKCa channel openers. Their synthesis from 2-chloro-3-nitropyridine is described together with their in vitro properties assessed by Rb-86(+) efflux and whole-cell patch-clamp assays using HEK293 cells stably transfected with the BKCa alpha subunit. In vitro functional characterization of BKCa channel opening activity was also assessed by measurement of relaxation of smooth muscle tissue strips obtained from Landrace pig bladders. The preliminary SAR data indicate the importance of steric bulk around the 2-amino substituent. (C) 2003 Elsevier Science Ltd. All rights reserved.

引用

页码：2003 / 2007

页数：5

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