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

Smail Khelili, Xavier Florence, Mourad Bouhadja, Samia Abdelaziz, Nadia Mechouch, Yekhlef Mohamed, Pascal de Tullio, Philippe Lebrun, Bernard Pirotte

文献索引：Bioorg. Med. Chem. 16(11) , 6124-30, (2008)

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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.