具有体外肝期抗疟原虫活性的新型方酸二酰胺
Novel squaramides with in vitro liver stage antiplasmodial activity.
作者信息
Ribeiro Carlos J A, Espadinha Margarida, Machado Marta, Gut Jiri, Gonçalves Lídia M, Rosenthal Philip J, Prudêncio Miguel, Moreira Rui, Santos Maria M M
机构信息
Research Institute for Medicines (iMed.ULisboa), Faculty of Pharmacy, Universidade de Lisboa, Av. Professor Gama Pinto, 1649-003 Lisboa, Portugal.
Instituto de Medicina Molecular, Faculdade de Medicina, Universidade de Lisboa, Av. Professor Egas Moniz, 1649-028 Lisboa, Portugal.
出版信息
Bioorg Med Chem. 2016 Apr 15;24(8):1786-92. doi: 10.1016/j.bmc.2016.03.005. Epub 2016 Mar 3.
A structure-activity relationship study was performed with ten 8-aminoquinoline-squaramides compounds active against liver stage malaria parasites, using human hepatoma cells (Huh7) infected by Plasmodium berghei parasites. In addition, their blood-schizontocidal activity was assessed against chloroquine-resistant W2 strain Plasmodium falciparum. Compound 3 was 7.3-fold more potent than the positive control primaquine against liver-stage parasites, illustrating the importance of the squarate moiety to activity.
利用被伯氏疟原虫感染的人肝癌细胞（Huh7），对十种对肝期疟原虫有活性的8-氨基喹啉方酰胺化合物进行了构效关系研究。此外，还评估了它们对氯喹耐药的恶性疟原虫W2株的血裂殖体杀灭活性。化合物3对肝期寄生虫的活性比阳性对照伯氨喹高7.3倍，说明了方酸部分对活性的重要性。
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