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抗疟化疗:青蒿素衍生二聚碳酸酯和硫代碳酸酯。

Antimalarial chemotherapy: artemisinin-derived dimer carbonates and thiocarbonates.

机构信息

Department of Chemistry, School of Arts and Sciences, The Johns Hopkins University, 3400 North Charles Street, Baltimore, MD 21218, United States.

W. Harry Feinstone Department of Molecular Microbiology and Immunology, Bloomberg School of Public Health, The Johns Hopkins University, Baltimore, MD 21205, United States; The Johns Hopkins Malaria Research Institute, Bloomberg School of Public Health, The Johns Hopkins University, Baltimore, MD 21205, United States.

出版信息

Bioorg Med Chem Lett. 2014 Jun 1;24(11):2440-3. doi: 10.1016/j.bmcl.2014.04.025. Epub 2014 Apr 16.

Abstract

Several 2-carbon-linked trioxane dimer secondary alcohol carbonates 14 and thiocarbonates 15, combined with mefloquine and administered in a low single oral dose, prolonged the survival times of malaria-infected mice much more effectively than the popular monomeric antimalarial drug artemether plus mefloquine. Three dimer carbonates 14 and one dimer thiocarbonate 15 partially cured malaria-infected mice.

摘要

几种 2-碳连接的三氧杂环己二酮二聚体仲醇碳酸酯 14 和硫代碳酸酯 15,与甲氟喹联合使用,以低单口服剂量给药,比流行的单体抗疟药青蒿琥酯加甲氟喹更有效地延长了感染疟疾的小鼠的存活时间。三种二聚碳酸酯 14 和一种二聚硫代碳酸酯 15 部分治愈了感染疟疾的小鼠。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/03cc/4074917/ebc8a50f1090/nihms591228f1.jpg

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