1,5-Diarylsubstituted 1,2,3-triazoles as potassium channel activators. VI.
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).
Biagi
Giuliana
G
Dipartimento di Scienze Farmaceutiche, via Bonanno 6, 56126 Pisa, Italy.
Calderone
Vincenzo
V
Giorgi
Irene
I
Livi
Oreste
O
Martinotti
Enrica
E
Martelli
Alma
A
Nardi
Antonio
A
D000818:Animals; D001562:Benzimidazoles; D020128:Inhibitory Concentration 50; D008956:Models, Chemical; D009126:Muscle Relaxation / Q000187:drug effects*; D009131:Muscle, Smooth, Vascular / Q000187:drug effects* / Q000502:physiology; D024681:Potassium Channels, Calcium-Activated / Q000378:metabolism*; D051381:Rats; D014230:Triazoles / Q000138:chemical synthesis / Q000494:pharmacology*; D014665:Vasodilator Agents / Q000138:chemical synthesis / Q000494:pharmacology*
D001562:Benzimidazoles; D024681:Potassium Channels, Calcium-Activated; D014230:Triazoles; D014665:Vasodilator Agents; C086491:NS 1619