喹啉基查尔酮的合成及其抗疟活性评估。
Synthesis of quinolinyl chalcones and evaluation of their antimalarial activity.
作者信息
Domínguez J N, Charris J E, Lobo G, Gamboa de Domínguez N, Moreno M M, Riggione F, Sanchez E, Olson J, Rosenthal P J
机构信息
Laboratorio de Síntesis Orgánica, Facultad de Farmacia, Universidad Central de Venezuela, 1051, Caracas, Venezuela.
出版信息
Eur J Med Chem. 2001 Jun;36(6):555-60. doi: 10.1016/s0223-5234(01)01245-4.
Quinolinyl chalcones were synthesized and evaluated for their inhibition of the Plasmodium falciparum cystein protease falcipain and their activity against cultured P. falciparum parasites. They were also tested for in vivo efficacy in a rodent P. berghei model. Their activity against falcipain and as antimalarials was moderate, but antimalarial activity was probably not due to the inhibition of falcipain and may follow a different mechanism. 1-(2,4-Dichlorophenyl)-3-[3-(2-chloro-6,7-dimethoxiquinolinyl)]-2-propen-1-one 3j was the most promising compound among those here reported (IC50 19.0 microM).
合成了喹啉基查尔酮，并评估了它们对恶性疟原虫半胱氨酸蛋白酶恶性疟原虫蛋白酶的抑制作用以及对培养的恶性疟原虫寄生虫的活性。还在啮齿动物伯氏疟原虫模型中测试了它们的体内疗效。它们对恶性疟原虫蛋白酶的活性和作为抗疟药的活性适中，但抗疟活性可能不是由于对恶性疟原虫蛋白酶的抑制，可能遵循不同的机制。1-(2,4-二氯苯基)-3-[3-(2-氯-6,7-二甲氧基喹啉基)]-2-丙烯-1-酮3j是本文报道的最有前景的化合物(IC50为19.0 microM)。
Zotero 插件