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High-throughput Screening for Small-molecule Modulators of Inward Rectifier Potassium Channels
Published on: January 27, 2013
1,4- and 2,4-substituted-1,2,3-triazoles as potential potassium channel activators. VII
Vincenzo Calderone1, Irene Giorgi, Oreste Livi
1Dipartimento di Psichiatria, Neurobiologia, Farmacologia e Biotecnologie, Facoltà di Farmacia, Università di Pisa, via Bonanno 6, I-56126 Pisa, Italy.
Abstract:
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.
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