Design and synthesis of novel 2-pyridone peptidomimetic falcipain 2/3 inhibitors

Bioorganic & Medicinal Chemistry Letters
2008.0

Abstract

The structure-based design, chemical synthesis and in vitro activity evaluation of various falcipain inhibitors derived from 2-pyridone are reported. These compounds contain a peptidomimetic binding determinant and a Michael acceptor terminal moiety capable of deactivating the cysteine protease active site.

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