Screening of Protease Inhibitors as Antiplasmodial Agents. Part I: Aziridines and Epoxides
ChemMedChem2007Vol. 2(8), pp. 1214–1224
Citations Over TimeTop 10% of 2007 papers
F. A. Schulz, Christoph Gelhaus, Björn Degel, Radim Vičík, Saskia Heppner, Alexander Breuning, Matthias Leippe, Jiří Gut, Philip J. Rosenthal, Tanja Schirmeister
Abstract
A broad protease-based and cell-based screening of protease inhibitors yielded the aziridine-2-carboxylic acid derivative 2 a and the N-acylated aziridine-2,3-dicarboxylic acid derivatives 32 a and 34 b as the most potent inhibitors of falcipain-2 and falcipain-3 (IC(50) falcipain-2: 0.079-5.4 microM, falcipain-3: 0.25-39.8 microM). As the compounds also display in vitro activity against the P. falciparum parasite in the submicromolar and low micromolar range, these compound classes are leads for new antiplasmodial falcipain inhibitors.
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