Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
8993461 | Il Farmaco | 2005 | 9 Pages |
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.
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Authors
Vincenzo Calderone, Irene Giorgi, Oreste Livi, Enrica Martinotti, Alma Martelli, Antonio Nardi,