Kitas Eric A, Löffler Bernd-Michael, Daetwyler Stefan, Dehmlow Henrietta, Aebi Johannes D
Pharma Division, Preclinical Research, F. Hoffmann-La Roche Ltd., CH-4070, Basel, Switzerland.
Bioorg Med Chem Lett. 2002 Jul 8;12(13):1727-30. doi: 10.1016/s0960-894x(02)00254-8.
The solid-phase synthesis of substituted 1,2,4-triazoles tethered to a 4-mercaptopyrrolidine core 1 is described. This novel class of non-peptidic, Zn(2+) metallo-protease inhibitors was found to have inhibitory activity for the endothelin converting enzyme (ECE-1). The SAR of the substitution pattern in 1 is discussed.
本文描述了与4-巯基吡咯烷核心1相连的取代1,2,4-三唑的固相合成。发现这类新型非肽类Zn(2+)金属蛋白酶抑制剂对内皮素转化酶（ECE-1）具有抑制活性。文中讨论了1中取代模式的构效关系。
