Institute for Molecular Bioscience, University of Queensland, Brisbane, Australia.
Bioorg Med Chem Lett. 2010 Jan 1;20(1):252-5. doi: 10.1016/j.bmcl.2009.10.122. Epub 2009 Oct 30.
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.
阿扎迪肽腈——新型半胱氨酸蛋白酶抑制剂——对氯喹敏感和氯喹耐药的培养疟原虫均显示出结构依赖性抗疟活性。还研究了对寄生虫血红蛋白降解半胱氨酸蛋白酶的抑制作用，结果表明阿扎迪肽腈是强效的falcipain-2 和 -3 抑制剂。观察到化合物的半胱氨酸蛋白酶抑制活性与抗疟潜力之间存在相关性。这些第一代阿扎迪肽腈代表了一类有前途的新型抗疟药物化合物。
