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

被引：5
|
作者：
Salerno, L.
Guerrera, F.
Modica, M.
Romeo, G.
Pittala, V.
Siracusa, M. A.
Mereghetti, I.
Cagnotto, A.
Mennini, T.
机构：
[1] Univ Catania, Dipartimento Sci Farmaceut, I-95125 Catania, Italy
[2] Ist Ric Farmacol Mario Negri, I-20157 Milan, Italy
来源：
MEDICINAL CHEMISTRY | 2007年 / 3卷 / 06期
关键词：
hypertension; endothelins; ET receptors; binding assays; 1,2,4-triazoles; regioisomers;
D O I：
10.2174/157340607782360281
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
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.
引用
收藏
页码：551 / 560
页数：10
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