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Mechanism-based design, synthesis, and in vitro antimalarial testing of new 4-methylated trioxanes structurally related to artemisinin: the importance of a carbon-centered radical for antimalarial activity.

作者信息

Posner G H, Oh C H, Wang D, Gerena L, Milhous W K, Meshnick S R, Asawamahasadka W

机构信息

Department of Chemistry, Johns Hopkins University, Baltimore, Maryland 21218.

出版信息

J Med Chem. 1994 Apr 29;37(9):1256-8. doi: 10.1021/jm00035a003.

DOI:10.1021/jm00035a003
PMID:8176702
Abstract
摘要

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Mechanism-based design, synthesis, and in vitro antimalarial testing of new 4-methylated trioxanes structurally related to artemisinin: the importance of a carbon-centered radical for antimalarial activity.基于机制的与青蒿素结构相关的新型4-甲基化三氧杂环已烷的设计、合成及体外抗疟测试:以碳为中心的自由基对抗疟活性的重要性
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[Recent advances in the study of artemisinin-related 1,2,4-trioxanes and ozonides (1,2,4-trioxolanes) as antimalarials].[作为抗疟药物的青蒿素相关1,2,4-三恶烷和臭氧化物(1,2,4-三恶戊烷)的研究新进展]
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Antimalarial cyclic peroxy ketals.
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Further evidence supporting the importance of and the restrictions on a carbon-centered radical for high antimalarial activity of 1,2,4-trioxanes like artemisinin.进一步的证据支持了以碳为中心的自由基对于青蒿素这类1,2,4-三恶烷的高抗疟活性的重要性及限制因素。
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Design, Synthesis, and Biological Evaluation of Novel 1,2,4-Trioxanes as Potential Antimalarial Agents.新型1,2,4-三氧杂环己烷作为潜在抗疟药物的设计、合成及生物学评价
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