Cipargamin

一种抗疟药；抑制野生型或突变型PfATP4的Na+-ATPase活性（恶性疟原虫膜中的IC50s分别为12.3-13.9和21.1-32.5nM）；对恶性疟原虫氯喹敏感株NF54和氯喹抗性株K1有效（IC50s分别为0.5和0.6nM）；在10、30和100mg/kg剂量下，可减少寄生虫血症并提高伯氏疟原虫感染小鼠模型的存活率。An antimalarial agent; inhibits the Na+-ATPase activity of wild-type or mutant PfATP4 (IC50s = 12.3-13.9 and 21.1-32.5 nM, respectively, in P. falciparum membranes); active against the P. falciparum chloroquine-sensitive strain NF54 and chloroquine-resistant strain K1 (IC50s = 0.5 and 0.6 nM, respectively); reduces parasitemia and increases survival in a mouse model of P. berghei infection at 10, 30, and 100 mg/kg.分子式C19H14Cl2FN3O分子量390.2FC1=C(C=C(C2=C1)NC3=C2C[C@@H](N[C@]34C5=C(NC4=O)C=CC(Cl)=C5)C)Cl