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Antimalarial activity of azadipeptide nitriles |
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| Authors: | Reik Löser Jiri Gut Philip J Rosenthal Maxim Frizler Michael Gütschow Katherine T Andrews |
| Institution: | 1. Institute for Molecular Bioscience, University of Queensland, Brisbane, Australia;2. School of Medicine, Division of Infectious Diseases, University of California at San Francisco, San Francisco, CA, USA;3. Pharmazeutisches Institut, Pharmazeutische Chemie I, Rheinische Friedrich-Wilhelms-Universität, Bonn, Germany;4. Eskitis Institute for Cell and Molecular Therapies, Griffith University, Nathan, Queensland, Australia;5. Queensland Institute for Medical Research, Herston, Queensland, Australia;6. Griffith Medical Research College, a joint program of Griffith University and QIMR, Herston, Queensland, Australia |
| Abstract: | Azadipeptide nitriles—novel cysteine protease inhibitors—display structure-dependent antimalarial activity against both chloroquine-sensitive and chloroquine-resistant lines of cultured Plasmodium falciparum malaria parasites. Inhibition of parasite’s hemoglobin-degrading cysteine proteases was also investigated, revealing the azadipeptide nitriles as potent inhibitors of falcipain-2 and -3. A correlation between the cysteine protease-inhibiting activity and the antimalarial potential of the compounds was observed. These first generation azadipeptide nitriles represent a promising new class of compounds for antimalarial drug development. |
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