新型抗疟苯基脲基查尔酮衍生物的合成与评价
Synthesis and evaluation of new antimalarial phenylurenyl chalcone derivatives.
作者信息
Domínguez José N, León Caritza, Rodrigues Juan, Gamboa de Domínguez Neira, Gut Jiri, Rosenthal Philip J
机构信息
Laboratorio de Síntesis Orgánica, Facultad de Farmacia, Universidad Central de Venezuela, Caracas, Venezuela.
出版信息
J Med Chem. 2005 May 19;48(10):3654-8. doi: 10.1021/jm058208o.
Phenylurenyl chalcone derivatives have been synthesized and tested as inhibitors of in vitro development of a chloroquine-resistant strain of Plasmodium falciparum, activity of the cysteine protease falcipain-2, in vitro globin hydrolysis, beta-hematin formation, and murine Plasmodium berghei malaria. The most active antimalarial compound was 1-[3'-N-(N'-phenylurenyl)phenyl]-3(3,4,5-trimethoxyphenyl)-2-propen-1-one 49, with an IC(50) of 1.76 microM for inhibition of P. falciparum development. Results suggest that chalcones exert their antimalarial activity via multiple mechanisms.
已合成苯基脲基查尔酮衍生物，并将其作为抗氯喹恶性疟原虫耐药株体外发育抑制剂、半胱氨酸蛋白酶恶性疟原虫蛋白酶-2活性抑制剂、体外珠蛋白水解抑制剂、β-血红素形成抑制剂以及鼠伯氏疟原虫疟疾抑制剂进行了测试。活性最强的抗疟化合物是1-[3'-N-(N'-苯基脲基)苯基]-3(3,4,5-三甲氧基苯基)-2-丙烯-1-酮49，其抑制恶性疟原虫发育的IC(50)为1.76微摩尔。结果表明，查尔酮通过多种机制发挥其抗疟活性。
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