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口服活性抗疟药：针对小鼠多药耐药疟疾的一系列新型甾体基1,2,4-三氧杂环己烷的合成与生物评价

Orally active antimalarials: synthesis and bioevaluation of a new series of steroid-based 1,2,4-trioxanes against multi-drug resistant malaria in mice.

作者信息

Singh Chandan, Sharma Upasana, Saxena Gunjan, Puri Sunil K

机构信息

Division of Medicinal and Process Chemistry, Central Drug Research Institute, Lucknow 226001, India.

出版信息

Bioorg Med Chem Lett. 2007 Aug 1;17(15):4097-101. doi: 10.1016/j.bmcl.2007.05.055. Epub 2007 May 23.

DOI:10.1016/j.bmcl.2007.05.055
PMID:17548195
Abstract

A new series of steroid-based 1,2,4-trioxanes 7a-f, 8a-f and 9b-e have been synthesized and evaluated for their antimalarial activity against multi-drug resistant Plasmodium yoelii in Swiss mice by oral route. The biological activity shows a strong dependence on the size and the nature of the steroidal side chain. Pregnane-based trioxanes 8a-f show better activity profile than trioxanes 7a-f and 9b-e, derived from cholesterol and tigogenine, respectively.

摘要

已经合成了一系列新的基于甾体的1,2,4 - 三恶烷7a - f、8a - f和9b - e，并通过口服途径对其在瑞士小鼠中针对多药耐药约氏疟原虫的抗疟活性进行了评估。生物活性显示出对甾体侧链大小和性质的强烈依赖性。基于孕烷的三恶烷8a - f显示出比分别源自胆固醇和替告皂甙元的三恶烷7a - f和9b - e更好的活性特征。

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