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

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

Volume: 3 Issue: 6

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

Affiliation:

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

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.

Cite this article as:

Salerno L., Guerrera F., Modica M., Romeo G., Pittala V., Siracusa A. M., Mereghetti I., Cagnotto A. and Mennini T., Synthesis of 1,2,4-triazole Derivatives: Binding Properties on Endothelin Receptors, Medicinal Chemistry 2007; 3 (6) . https://dx.doi.org/10.2174/157340607782360281