Antimalarial activity of azadipeptide nitriles

作者：Loeser Reik; Gut Jiri; Rosenthal Philip J; Frizler Maxim; Guetschow Michael; Andrews Katherine T

来源：Bioorganic & Medicinal Chemistry Letters, 2010, 20(1): 252-255.

DOI：10.1016/j.bmcl.2009.10.122

• Malaria
• Azadipeptide nitriles
• P. falciparum
• Falcipains
• Cysteine protease inhibitors

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.

• 出版日期2010-1-1
• 单位河北医科大学