Structure-activity relationship of a novel class of naphthyl amide KATP channel openers

被引：8

作者：

Turner, SC

Carroll, WA

White, TK

Brune, ME

Buckner, SA

Gopalakrishnan, M

Fabiyi, A

Coghlan, MJ

Scott, VE

Castle, NA

Daza, AV

Milicic, I

Sullivan, JP

机构：

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

[2] Icagen Inc, Durham, NC 27703 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 10期

关键词：

D O I：

10.1016/S0960-894X(03)00205-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We have discovered a novel series of N-[2-(2,2,2-trifluoro-1-hydroxy-1-trifluoromethyl-ethyl)-naphthalen-1-yl] amides that are potent openers of K-ATP channels and investigated structure-activity relationships (SAR) around the 1,2-disubstituted naphthyl core. A-151892, a prototype compound of this series, was found to be a potent and efficacious potassium channel opener in vitro in transfected Kir6.2/SUR2B cells and pig bladder strips. Additionally, A-151892 was found to selectively inhibit unstable bladder contractions in vivo in an obstructed rat model of myogenic bladder function. (C) 2003 Elsevier Science Ltd. All rights reserved.

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收藏

页码：1741 / 1744

页数：4

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