Two 2-hydroxy-3-alkyl-1,4-naphthoquinones with in vitro and in vivo activities against Toxoplasma gondii.
Two 2-hydroxy-3-alkyl-1,4-naphthoquinones with in vitro and in vivo activities against Toxoplasma gondii.
复制标题
两个 2-羟基-3-烷基-1,4-萘醌具有体外和体内抗弓形虫活性。
DOI：
10.1128/aac.42.9.2284
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发表时间：
1998
影响因子：
4.9
通讯作者：
Araujo,FG
中科院分区：
文献类型：
--
作者：
Khan,AA;Nasr,M;Araujo,FG
本文研究了两种3-烷基取代的2-羟基-1，4-萘醌类化合物NSC 113452（NSC 52）和NSC 113455（NSC 55）在体外和小鼠急性弓形虫病模型中的抗弓形虫活性。在体外，NSC 52和NSC 55均显著抑制T.刚地。在体内，每种化合物单独和与目前用于治疗人弓形虫病的其他药物组合进行检查。虽然口服给药时，没有一种化合物能保护小鼠免于死亡，但当腹腔内给药时，两者都具有显著的保护作用。此外，当每种化合物的次优剂量与次优剂量的乙胺嘧啶或磺胺嘧啶组合使用时，观察到存活率显著增加。这些结果表明，NSC 52或NSC 55与乙胺嘧啶或磺胺嘧啶的组合具有有希望的抗T活性。刚地。
Two 3-alkyl-substituted 2-hydroxy-1,4-naphthoquinones, NSC 113452 (NSC52) and NSC 113455 (NSC55), were evaluated for activity againstToxoplasma gondiiin vitro and in murine models of acute toxoplasmosis. In vitro, both NSC52 and NSC55 significantly inhibited intracellular replication ofT. gondii. In vivo, each compound was examined alone and in combination with other drugs currently used for treatment of human toxoplasmosis. Although none of the compounds protected mice against death when administered orally, both were significantly protective when administered intraperitoneally. In addition, a significant increase in survival was observed when suboptimal doses of each compound were used in combination with suboptimal doses of pyrimethamine or sulfadiazine. These results indicate that combinations of NSC52 or NSC55 with pyrimethamine or sulfadiazine have promising activity againstT. gondii.