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

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

Bioorganic & medicinal chemistry (2008-05-16)
Smail Khelili, Xavier Florence, Mourad Bouhadja, Samia Abdelaziz, Nadia Mechouch, Yekhlef Mohamed, Pascal de Tullio, Philippe Lebrun, Bernard Pirotte
RESUMO

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.

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Sigma-Aldrich
3-Cyanophenyl isocyanate, 97%