Abstract
We disclose here for the first time the curative activity of a new generation of trioxane dimers, designed logically and prepared easily from the natural trioxane artemisinin in only four or five chemical steps that would be easily accomplished also on a manufacturing scale. Four of these trioxane dimers cure malaria-infected mice after only a single subcutaneous dose, and two other dimers cure after three oral doses.
Publication types
-
Research Support, N.I.H., Extramural
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Animals
-
Antimalarials / chemical synthesis*
-
Antimalarials / chemistry
-
Antimalarials / therapeutic use
-
Artemisinins / chemical synthesis*
-
Artemisinins / chemistry
-
Artemisinins / therapeutic use
-
Bridged Bicyclo Compounds, Heterocyclic / chemical synthesis*
-
Bridged Bicyclo Compounds, Heterocyclic / chemistry
-
Bridged Bicyclo Compounds, Heterocyclic / therapeutic use
-
Malaria / drug therapy*
-
Malaria / mortality
-
Mice
-
Plasmodium berghei
-
Structure-Activity Relationship
Substances
-
Antimalarials
-
Artemisinins
-
Bridged Bicyclo Compounds, Heterocyclic