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Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1573-4064
ISSN (Online): 1875-6638

Synthesis of 1,2,4-triazole Derivatives: Binding Properties on Endothelin Receptors

Author(s): L. Salerno, F. Guerrera, M. Modica, G. Romeo, V. Pittala, M. A. Siracusa, I. Mereghetti, A. Cagnotto and T. Mennini

Volume 3, Issue 6, 2007

Page: [551 - 560] Pages: 10

DOI: 10.2174/157340607782360281

Price: $65

Abstract

In the present study we describe the synthesis of a new series of 1,2,4-triazoles: [3-(arylmethyl)thio-5-aryl-4H- [1,2,4]triazol-4-yl]acetic acids 5a-g, [5-(arylmethyl)thio-3-aryl-1H-[1,2,4]triazol-1-yl]acetic acids 8a-d, and [3-(arylmethyl) thio-5-aryl-1H-[1,2,4]triazol-1-yl] acetic acids 9a-d. These compounds were tested in binding assays to evaluate their ability as ligands for human ETA and ETB receptors stably expressed in CHO cells; some of the tested compounds showed affinity in the micromolar range.

Keywords: Hypertension, endothelins, ET receptors, binding assays, 1,2,4-triazoles, regioisomers


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