Salerno L, Guerrera F, Modica M, Romeo G, Pittalà V, Siracusa M A, Mereghetti I, Cagnotto A, Mennini T
Dipartimento di Scienze Farmaceutiche, Università degli Studi di Catania, viale A. Doria, 6, 95125 Catania, Italy.
Med Chem. 2007 Nov;3(6):551-60. doi: 10.2174/157340607782360281.
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.
在本研究中，我们描述了一系列新的1,2,4 - 三唑的合成：[3 -（芳基甲基）硫代 - 5 - 芳基 - 4H - [1,2,4]三唑 - 4 - 基]乙酸5a - g、[5 -（芳基甲基）硫代 - 3 - 芳基 - 1H - [1,2,4]三唑 - 1 - 基]乙酸8a - d以及[3 -（芳基甲基）硫代 - 5 - 芳基 - 1H - [1,2,4]三唑 - 1 - 基]乙酸9a - d。这些化合物在结合试验中进行了测试，以评估它们作为稳定表达于CHO细胞中的人ET(A)和ET(B)受体配体的能力；一些测试化合物在微摩尔范围内显示出亲和力。
