New 1,4- and 2,4-substituted 1,2,3-triazole derivatives were synthesized and tested as potential BKCa channel openers, as a part of a research program, which hypothesizes a pharmacophoric structure containing the 1,2,3-triazole ring. The structure–activity relationships were studied introducing some structural changes concerning molecular geometry and the presence of a hydrogen bond donor as a primary amino group and a phenolic or alcoholic hydroxy function. The compounds were prepared by nucleophilic substitution on the 1,2,3-triazole ring and by 1,3-dipolar cycloaddition of azides to selected alkynes and to phenylacetone. The new compounds tested on rat aortic rings did not exhibit any significant vasorelaxing activity.
|Autori interni:||CALDERONE, VINCENZO|
|Autori:||V. CALDERONE; GIORGI I; O. LIVI; E. MARTINOTTI; A. MARTELLI; A. NARDI|
|Titolo:||1,4- and 2,4-substituted-1,2,3-triazoles as potential potassium channel activators. VII.|
|Anno del prodotto:||2005|
|Digital Object Identifier (DOI):||10.1016/j.farmac.2005.03.004|
|Appare nelle tipologie:||1.1 Articolo in rivista|