Synthesis of triazole-Tethered pyrrolidine libraries: novel ECE inhibitors |
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| Authors: | Kitas Eric A Löffler Bernd-Michael Daetwyler Stefan Dehmlow Henrietta Aebi Johannes D |
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| Institution: | Pharma Division, Preclinical Research, F. Hoffmann-La Roche Ltd., CH-4070, Basel, Switzerland. eric_a.kitas@roche.com |
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| Abstract: | 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. |
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