ANTIMALARIAL SULFONE TRIOXANES

Authors
POSNER GH ODOWD H CAFERRO T CUMMING JN PLOYPRADITH P XIE SJ SHAPIRO TA
Citation
Gh. Posner et al., ANTIMALARIAL SULFONE TRIOXANES, Tetrahedron letters, 39(16), 1998, pp. 2273-2276
Citations number
30
Categorie Soggetti
Chemistry Inorganic & Nuclear
Journal title
Tetrahedron letters → ACNP
ISSN journal
00404039
Volume
39
Issue
16
Year of publication
1998
Pages
2273 - 2276
Database
ISI
SICI code
0040-4039(1998)39:16<2273:AST>2.0.ZU;2-L
Abstract
A series of new sulfide and sulfone 1,2,4-trioxanes was prepared in on ly a few steps from commercial reactants. The sulfone trioxanes were f ound 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 po tent as the complex natural antimalarial trioxane artemisinin (2). A t entative chemical mechanism is proposed to account for the great diffe rence in antimalarial activity of the 12 alpha-vs. 12 beta-sulfide tri oxanes. (C) 1998 Elsevier Science Ltd. All rights reserved.