The synthesis and biological evaluation of a range of novel functionalised benzopyrans as potential potassium channel activators

被引：13

作者：

Tyrrell, Elizabeth ^{[1
]}

Tesfa, Kibur Hunie ^{[1
]}

Greenwood, Iain ^{[2
]}

Mann, Alistair ^{[1
]}

机构：

[1] Kingston Univ, Sch Pharm & Chem, Kingston upon Thames KT1 2EE, Surrey, England

[2] Univ London, London SW17 0RE, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 03期

关键词：

benzopyrans; Nicholas reaction; chiral; potassium channel activators; cromakalim; rat thoracic tissue; smooth muscle relaxation;

D O I：

10.1016/j.bmcl.2007.11.135

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A range of novel benzopyrans have been synthesised and biologically evaluated for K-ATP channel activity employing cromakalim 1 as a benchmark K-ATP channel opener. Although the compounds that were evaluated demonstrated a reduced ability to relax phenylephrine stimulated rat thoracic tissue, we provide evidence that benzopyrans 7a-h may be operating via an alternative mechanism than ATP-sensitive K+ channel activity. (C) 2008 Published by Elsevier Ltd.

引用

页码：1237 / 1240

页数：4