1,4- and 2,4-substituted-1,2,3-triazoles as potential potassium channel activators. VII.
New 1,4- and 2,4-substituted 1,2,3-triazole derivatives were synthesized and tested as potential BK(Ca) 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.
Calderone
Vincenzo
V
Dipartimento di Psichiatria, Neurobiologia, Farmacologia e Biotecnologie, Facoltà di Farmacia, Università di Pisa, via Bonanno 6, I-56126 Pisa, Italy.
Giorgi
Irene
I
Livi
Oreste
O
Martinotti
Enrica
E
Martelli
Alma
A
Nardi
Antonio
A
D000818:Animals; D002626:Chemistry, Pharmaceutical / Q000379:methods; D015221:Potassium Channels / Q000819:agonists*; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
D015221:Potassium Channels; D014230:Triazoles