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首页> 外文期刊>Journal of Medicinal Chemistry >New orally active derivatives of artemisinin with high efficacy against multidrug-resistant malaria in mice
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New orally active derivatives of artemisinin with high efficacy against multidrug-resistant malaria in mice

机译：青蒿素的新型口服活性衍生物，对小鼠的多重耐药性疟疾具有高疗效

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摘要

A new series of ether derivatives of dihydroartemisinin have been prepared and evaluated for their antimalarial activity against multidrug-resistant Plasmodium yoelii nigeriensis in mice by oral route. These new derivatives 7-17 are highly lipophilic ( log P in the range of 5.51 to 7.19) as compared with beta-arteether (log P 3.84), and several of them are two- to four-fold more active than beta-arteether. Among the ether derivatives, R-isomers are more active than the beta- isomers. The ether derivatives 12 alpha and 14 alpha, the most active compounds of the series, provided 100% protection to infected mice at 12 mg/kg x 4 days. In this model,- arteether provides 100% and 20% protection at 48 mg/kg x 4 days and 24 mg/kg x 4 days, respectively.
机译：制备了一系列新的双氢青蒿素醚衍生物，并通过口服途径评价了它们对小鼠多药耐药性约氏疟原虫的抗疟活性。这些新衍生物7-17与β-蒿甲醚（对数P 3.84）相比，具有高度亲脂性（log P在5.51至7.19范围内），其中一些的活性是β-蒿甲醚的2至4倍。在醚衍生物中，R-异构体比β-异构体更具活性。该系列中活性最高的醚衍生物12 alpha和14 alpha以12 mg / kg x 4天的剂量为受感染的小鼠提供100％的保护。在该模型中，arteether分别在48 mg / kg x 4天和24 mg / kg x 4天时提供100％和20％的保护。

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