Synthesis of 1,2,4-triazole derivatives: Binding properties on endothelin receptors

L. Salerno, F. Guerrera, M. Modica, G. Romeo, V. Pittalà, M. A. Siracusa, I. Mereghetti, A. Cagnotto, T. Mennini

Research output: Contribution to journalArticlepeer-review

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-y1]acetic acids 5a-g, [5-(arylmethyl)thio-3-aryl-1H-[1,2,4]triazol-1-y1]acetic acids 8a-d, and [3-(aryl-methyl) thio-5-aryl-1H-[1,2,4]triazol-1-y1] 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.

Original languageEnglish
Pages (from-to)551-560
Number of pages10
JournalMedicinal Chemistry
Volume3
Issue number6
DOIs
Publication statusPublished - Nov 2007

Keywords

  • 1,2,4-triazoles
  • Binding assays
  • Endothelins
  • ET receptors
  • Hypertension
  • Regioisomers

ASJC Scopus subject areas

  • Drug Discovery

Fingerprint Dive into the research topics of 'Synthesis of 1,2,4-triazole derivatives: Binding properties on endothelin receptors'. Together they form a unique fingerprint.

Cite this