作者:Gary H. Posner、Hardwin O'Dowd、Thomas Caferro、Jared N. Cumming、Poonsakdi Ploypradith、Suji Xie、Theresa A. Shapiro
DOI:10.1016/s0040-4039(98)00290-1
日期:1998.4
A series of new sulfide and sulfone 1,2,4-trioxanes was prepared in only a few steps from commercial reactants. The sulfone trioxanes were found to have higher in vitro antimalarial potencies than the sulfides, with 12 beta-arylsulfone trioxanes 1 beta being from 1/3 to 1/4 as potent as the complex natural antimalarial trioxane artemisinin (2). A tentative chemical mechanism is proposed to account for the great difference in antimalarial activity of the 12 alpha-vs. 12 beta-sulfide trioxanes. (C) 1998 Elsevier Science Ltd. All rights reserved.