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.

Permalink: https://www.hzdr.de/publications/Publ-15014
Publ.-Id: 15014