As part of our program toward designing potassium channel openers, synthesis of a novel series of 1,5-diphenylsubstituted 1,2,3-triazoles, as potential activators of the large-conductance calcium-activated potassium channels (BK), as well as their vasorelaxant activity are presented. The functional effect of these potential structurally novel BK-openers on vascular contractile function were studied in vitro, using isolated rat aortic rings pre-contracted with KCl 20 mM. Among the target compounds, only 16 showed appreciable effectiveness, exhibiting an efficacy parameter (57%) lower than that of NS1619 and a comparable potency index (pIC50: 5.58). Z9 30
1,5-Diarylsubstituted 1,2,3-triazoles as potential potassium channels activators. VI.
CALDERONE, VINCENZO;GIORGI, IRENE;MARTELLI, ALMA;
2004-01-01
Abstract
As part of our program toward designing potassium channel openers, synthesis of a novel series of 1,5-diphenylsubstituted 1,2,3-triazoles, as potential activators of the large-conductance calcium-activated potassium channels (BK), as well as their vasorelaxant activity are presented. The functional effect of these potential structurally novel BK-openers on vascular contractile function were studied in vitro, using isolated rat aortic rings pre-contracted with KCl 20 mM. Among the target compounds, only 16 showed appreciable effectiveness, exhibiting an efficacy parameter (57%) lower than that of NS1619 and a comparable potency index (pIC50: 5.58). Z9 30I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
