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N-苄氧基二氢三嗪类似物:对恶性疟原虫的体外抗疟活性

Analogues of N-benzyloxydihydrotriazines: in vitro antimalarial activity against Plasmodium falciparum.

作者信息

Childs G E, Lambros C

出版信息

Ann Trop Med Parasitol. 1986 Apr;80(2):177-81. doi: 10.1080/00034983.1986.11812002.

DOI:10.1080/00034983.1986.11812002
PMID:3530157
Abstract

The antimalarial activities of a series of chlorophenyloxyalkoxy and chlorophenalkoxy N-substituted diamino-dihydrotriazines were determined in vitro against three strains of Plasmodium falciparum (Malayan Camp, Vietnam Smith, FCB) with diverse levels of resistance to chloroquine, pyrimethamine, and cycloguanil. Parasite viability was assayed by the inhibition of the uptake of radiolabelled hypoxanthine. Most of the ID-50S of these compounds were less than 1.0 ng ml-1. Consistent differences in sensitivities to these compounds were observed and appeared to be strain related. The Malayan Camp was the most sensitive and Vietnam Smith was the least sensitive. These differences appeared to be related primarily to an inherent sensitivity of a particular strain to the series of analogues examined rather than to a pattern of cross-resistance to chloroquine, pyrimethamine, or cycloguanil.

摘要

测定了一系列氯苯氧基烷氧基和氯苯烷氧基N-取代二氨基二氢三嗪对三株恶性疟原虫(马来亚营地株、越南史密斯株、FCB株)的体外抗疟活性,这三株疟原虫对氯喹、乙胺嘧啶和环氯胍具有不同程度的抗性。通过抑制放射性标记次黄嘌呤的摄取来测定寄生虫的活力。这些化合物的大多数半数抑制浓度(ID-50)小于1.0纳克/毫升。观察到对这些化合物的敏感性存在一致差异,且似乎与菌株有关。马来亚营地株最敏感,越南史密斯株最不敏感。这些差异似乎主要与特定菌株对所检测的一系列类似物的固有敏感性有关,而不是与对氯喹、乙胺嘧啶或环氯胍的交叉抗性模式有关。

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