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Synthesis of triazole-Tethered pyrrolidine libraries: novel ECE inhibitors
Eric A Kitas1, Bernd-Michael Löffler, Stefan Daetwyler
1Pharma Division, Preclinical Research, F. Hoffmann-La Roche Ltd., CH-4070, Basel, Switzerland. eric_a.kitas@roche.com
Bioorganic & Medicinal Chemistry Letters
|June 18, 2002
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.