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

共 50 条

[1] Potassium channel activators (KCAs):: 6-oxyderivatives of benzopyrans, synthesis and pharmacological properties
Weichel, C
Weber, C
Uhrig, U
Höltje, HD
Mannhold, R
Lemoine, H
NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY, 1998, 358 (01) : R697 - R697
[2] 6-oxyderivatives of benzopyrans as potassium channel activators (KCAs):: Synthesis and pharmacological properties
Weichel, C
Uhrig, U
Lemoine, H
Weber, H
Höltje, HD
Mannhold, R
NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY, 1998, 357 (04) : R77 - R77
[3] Synthesis and biological activity of novel substituted benzanilides as potassium channel activators. V
Biagi, G
Giorgi, I
Livi, O
Nardi, A
Calderone, V
Martelli, A
Martinotti, E
Salerni, OL
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2004, 39 (06) : 491 - 498
[4] 6-substituted benzopyrans as potassium channel activators: Synthesis, vasodilator properties, and multivariate analysis
Mannhold, R
Cruciani, G
Weber, H
Lemoine, H
Derix, A
Weichel, C
Clementi, M
JOURNAL OF MEDICINAL CHEMISTRY, 1999, 42 (06) : 981 - 991
[5] Design,synthesis and biological evaluation of novel glucokinase activators
Yong Qiang Li~a
ChineseChemicalLetters, 2011, 22 (01) : 73 - 76
[6] Discovery, synthesis and biological evaluation of novel glucokinase activators
McKerrecher, D
Allen, JV
Bowker, SS
Boyd, S
Caulkett, PWR
Currie, GS
Davies, CD
Fenwick, ML
Gaskin, H
Grange, E
Hargreaves, RB
Hayter, BR
James, R
Johnson, KM
Johnstone, C
Jones, CD
Lackie, S
Rayner, JW
Walker, RP
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2005, 15 (08) : 2103 - 2106
[7] Design, synthesis and biological evaluation of novel glucokinase activators
Li, Yong Qiang
Zhang, Yu Liang
Hu, Sheng Quan
Wang, Yu Ling
Song, Hong Rui
Feng, Zhi Qiang
Lei, Lei
Liu, Quan
Shen, Zhu Fang
CHINESE CHEMICAL LETTERS, 2011, 22 (01) : 73 - 76
[8] NOVEL SUBSTITUTED THIENOPYRANS AS A NEW FAMILY OF POTASSIUM CHANNEL ACTIVATORS
PRESS, JB
MCNALLY, JJ
SANFILIPPO, PJ
URBANSKI, M
FALOTICO, R
KATZ, L
GIARDINO, E
MOORE, JM
FASEB JOURNAL, 1992, 6 (04): : A1292 - A1292
[9] POTASSIUM CHANNEL ACTIVATORS - SYNTHESIS AND SAR STUDIES OF NOVEL 1,4-BENZOXAZINE DERIVATIVES
MATSUMOTO, Y
TSUZUKI, R
MATSUHISA, A
TAKAYAMA, K
YODEN, T
UCHIDA, W
ASANO, M
FUJITA, S
YANAGISAWA, I
FUJIKURA, T
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 1991, 202 : 99 - MEDI
[10] Diversity-oriented synthesis of marine polybrominated diphenyl ethers as potential KCNQ potassium channel activators
Liu, Lai-Xin
Gu, Ru-Rong
Jin, Yang
Chen, Xue-Qin
Li, Xu-Wen
Zheng, Yue-Ming
Gao, Zhao-Bing
Guo, Yue-Wei
BIOORGANIC CHEMISTRY, 2022, 126

← 1 2 3 4 5 →