title: 1,5-Diarylsubstituted 1,2,3-triazoles as potassium channel activators. VI.
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).
authors.affiliation: Dipartimento di Scienze Farmaceutiche, via Bonanno 6, 56126 Pisa, Italy.
authors.forename: Giuliana
authors.initials: G
authors.lastname: Biagi
authors.forename: Vincenzo
authors.initials: V
authors.lastname: Calderone
authors.forename: Irene
authors.initials: I
authors.lastname: Giorgi
authors.forename: Oreste
authors.initials: O
authors.lastname: Livi
authors.forename: Enrica
authors.initials: E
authors.lastname: Martinotti
authors.forename: Alma
authors.initials: A
authors.lastname: Martelli
authors.forename: Antonio
authors.initials: A
authors.lastname: Nardi
mesh_terms: 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*
chemical_list: D001562:Benzimidazoles; D024681:Potassium Channels, Calcium-Activated; D014230:Triazoles; D014665:Vasodilator Agents; C086491:NS 1619