A series of 1-aryl-6,7-disubstituted-2H-isoquinolin-3-ones (2–10) was synthesized and evaluated for their inhibition against Plasmodium falciparum cysteine protease falcipain-2, as well as against cultured P. falciparum strain FCBR parasites. All compounds displayed inhibitory activity against recombinant falcipain-2 and against in vitro cultured intraerythrocytic P. falciparum, with the exception of 9. The new compounds exhibited no selectivity against human cysteine proteases such as cathepsins B and L. The inhibitory activity of the synthesized compounds was also evaluated against another protozoal cysteine protease, namely rhodesain of Trypanosoma brucei rhodesiense.

合成了一系列的1-芳基-6,7-二取代-2 H-异喹啉-3-酮（2-10）并评估了其对恶性疟原虫半胱氨酸蛋白酶falcipain-2以及培养的恶性疟原虫的抑制作用。菌株FCBR寄生虫。除9以外，所有化合物均显示出对重组falcipain-2和体外培养的红细胞内恶性疟原虫的抑制活性。新化合物对人半胱氨酸蛋白酶（例如组织蛋白酶B和L）没有选择性。还评估了合成化合物对另一种原生动物半胱氨酸蛋白酶（即布鲁氏锥虫的罗氏菌素）的抑制活性。。