Synthesis and activity on rat aorta rings and rat pancreatic beta-cells of ring-opened analogues of benzopyran-type potassium channel activators.
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.
Khelili
Smail
S
Laboratoire de chimie pharmaceutique, de pharmacologie et d'ecotoxicologie, Faculté des sciences, Université de Jijel, B.P. 98 Ouled Aissa, 18000 Jijel, Algeria.
Florence
Xavier
X
Bouhadja
Mourad
M
Abdelaziz
Samia
S
Mechouch
Nadia
N
Mohamed
Yekhlef
Y
de Tullio
Pascal
P
Lebrun
Philippe
P
Pirotte
Bernard
B
D000818:Animals; D001011:Aorta / Q000187:drug effects* / Q000378:metabolism*; D001578:Benzopyrans / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002839:Chromans / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D019806:Cromakalim / Q000031:analogs & derivatives* / Q000494:pharmacology; D066298:In Vitro Techniques; D007328:Insulin / Q000378:metabolism; D007329:Insulin Antagonists / Q000138:chemical synthesis / Q000494:pharmacology; D000078790:Insulin Secretion; D050417:Insulin-Secreting Cells / Q000187:drug effects* / Q000378:metabolism*; D009126:Muscle Relaxation / Q000187:drug effects; D015221:Potassium Channels / Q000378:metabolism*; D051381:Rats; D017208:Rats, Wistar
D001578:Benzopyrans; D002839:Chromans; D007328:Insulin; D007329:Insulin Antagonists; D015221:Potassium Channels; D019806:Cromakalim