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Synthesis of 1,2,4-triazole derivatives: binding properties on endothelin receptors
L Salerno1, F Guerrera, M Modica
1Dipartimento di Scienze Farmaceutiche, Università degli Studi di Catania, viale A. Doria, 6, 95125 Catania, Italy. l.salerno@unict.it
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-(aryl-methyl)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 ET(A) and ET(B) receptors stably expressed in CHO cells; some of the tested compounds showed affinity in the micromolar range.
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