Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1372467 | Bioorganic & Medicinal Chemistry Letters | 2010 | 4 Pages |
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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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Reik Löser, Jiri Gut, Philip J. Rosenthal, Maxim Frizler, Michael Gütschow, Katherine T. Andrews,