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 language | English |
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Pages (from-to) | 551-560 |
Number of pages | 10 |
Journal | Medicinal Chemistry |
Volume | 3 |
Issue number | 6 |
DOIs | |
Publication status | Published - Nov 2007 |
Keywords
- 1,2,4-triazoles
- Binding assays
- Endothelins
- ET receptors
- Hypertension
- Regioisomers
ASJC Scopus subject areas
- Drug Discovery