8-（1-萘-2-基乙烯基）-6,7,10-三氧杂螺[4.5]癸烷，一种对啮齿动物和猿类疟疾有效的新型1,2,4-三恶烷。

8-(1-Naphthalen-2-yl-vinyl)-6,7,10-trioxaspiro (4.5) decane, a new 1,2,4-trioxane effective against rodent and simian malaria.

作者信息

Singh Chandan, Kanchan Rani, Srivastava Divya, 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. 2006 Feb;16(3):584-6. doi: 10.1016/j.bmcl.2005.10.044. Epub 2005 Nov 4.

DOI:10.1016/j.bmcl.2005.10.044

PMID:16275088

Abstract

A new series of 8-(1-aryl-vinyl)-6,7,10-trioxaspiro [4.5] decanes 7a-e and 3-(1-aryl-vinyl)-l,2,5-trioxaspiro [5.5] undecanes 8a-e have been prepared and screened against multi-drug resistant Plasmodium yoelii in mice. 8-(1-Naphthalen-2-yl-vinyl)-6,7,10-trioxaspiro [4.5] decane 7b, the most active trioxane of the series, has also shown promising activity against Plasmodium cynomolgi in rhesus monkeys.

摘要

已制备出一系列新的8-(1-芳基乙烯基)-6,7,10-三氧杂螺[4.5]癸烷7a-e和3-(1-芳基乙烯基)-1,2,5-三氧杂螺[5.5]十一烷8a-e，并在小鼠体内针对多药耐药性约氏疟原虫进行了筛选。该系列中活性最高的三恶烷8-(1-萘-2-基乙烯基)-6,7,10-三氧杂螺[4.5]癸烷7b，在恒河猴体内对食蟹猴疟原虫也显示出有前景的活性。