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.

1,4- and 2,4-substituted-1,2,3-triazoles as potential potassium channel activators. VII.

CALDERONE, VINCENZO;GIORGI, IRENE;MARTELLI, ALMA;
2005-01-01

Abstract

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.
Calderone, Vincenzo; Giorgi, Irene; O., Livi; E., Martinotti; Martelli, Alma; A., Nardi
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11568/181982
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