Synthesis and activity on rat aorta rings and rat pancreatic β-cells of ring-opened analogues of benzopyran-type potassium channel activators

被引：23

作者：

Khelili, Smail ^{[2
]}

Florence, Xavier ^{[1
]}

Bouhadja, Mourad ^{[2
]}

Abdelaziz, Samia ^{[2
]}

Mechouch, Nadia ^{[2
]}

Mohamed, Yekhlef ^{[2
]}

de Tullio, Pascal ^{[1
]}

Lebrun, Philippe ^{[3
]}

Pirotte, Bernard ^{[1
]}

机构：

[1] Univ Liege, CHU, Ctr Interfac Rech Medicament, Lab Chim Pharmaceut, B-4000 Liege, Belgium

[2] Univ Jijel, Fac Sci, Lab Chim Pharmaceut Pharmacol & Ecotoxicol, Jijel 18000, Algeria

[3] Univ Libre Bruxelles, Fac Med, Lab Pharmacodynamie & Therapeut, B-1070 Brussels, Belgium

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2008年 / 16卷 / 11期

关键词：

ring-opened cromakalim analogues; inhibition of insulin secretion; vasorelaxant effect; potassium channel opener;

D O I：

10.1016/j.bmc.2008.04.043

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Ring-opened analogues of dihydrobenzopyran potassium channel openers (PCOs) were prepared and evaluated as putative PCOs on rat aorta rings (myorelaxant effect) and rat pancreatic beta-cells (inhibition of insulin secretion). These derivatives are characterized by the presence of a sulfonylurea, a urea or an amide function. Some compounds bearing an arylurea moiety provoked vasorelaxant effects and a marked inhibition of insulin release. Derivatives bearing a sulfonylurea or an amide function were, however, poorly active on both tissues. Structure-activity relationships and apparent tissue selectivity are discussed. (C) 2008 Elsevier Ltd. All rights reserved.

引用

页码：6124 / 6130

页数：7