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ID: ALA1138088

Journal: Bioorg Med Chem Lett

Title: Design and synthesis of selective keto-1,2,4-oxadiazole-based tryptase inhibitors.

Authors: Palmer JT, Rydzewski RM, Mendonca RV, Sperandio D, Spencer JR, Hirschbein BL, Lohman J, Beltman J, Nguyen M, Liu L.

Abstract: Using a scaleable, directed library approach based on orthogonally protected advanced intermediates, we have prepared a series of potent keto-1,2,4-oxadiazoles designed to explore the P(2) binding pocket of human mast cell tryptase, while building in a high degree of selectivity over human trypsin and other serine proteases.

CiteXplore: 16644215

DOI: 10.1016/j.bmcl.2006.04.013