Antimalarial activity of azadipeptide nitriles
Antimalarial activity of azadipeptide nitriles
Löser, R.; Gut, J.; Rosenthal, P. J.; Frizler, M.; Gütschow, M.; Andrews, K. T.
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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Bioorganic & Medicinal Chemistry Letters 20(2010), 252-255
DOI: 10.1016/j.bmcl.2009.10.122
Cited 11 times in Scopus
Permalink: https://www.hzdr.de/publications/Publ-15014
Publ.-Id: 15014