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 , T. Mennini .

Journal Name: Medicinal Chemistry

Volume 3 , Issue 6 , 2007

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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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Article Details

VOLUME: 3
ISSUE: 6
Year: 2007
Page: [551 - 560]
Pages: 10
DOI: 10.2174/157340607782360281
Price: $58

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