Abstract
Sixteen new anilide derivatives of the natural trioxane artemisinin were prepared and evaluated for antimalarial efficacy in Plasmodium berghei infected mice. Of these 16 new anilides administered orally as one 6 mg/kg dose combined with 18 mg/kg mefloquine hydrochloride, only sulfide 3-arteSanilide 12d was completely curative: on day 30 after infection, all mice in this group had no detectable parasitemia, gained as much weight as the uninfected control mice, and behaved normally.
Publication types
-
Research Support, N.I.H., Extramural
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Administration, Oral
-
Anilides / chemical synthesis*
-
Anilides / chemistry
-
Anilides / therapeutic use
-
Animals
-
Antimalarials / chemical synthesis*
-
Antimalarials / chemistry
-
Antimalarials / therapeutic use
-
Drug Therapy, Combination
-
Malaria / drug therapy*
-
Mefloquine / therapeutic use*
-
Mice
-
Parasitemia / drug therapy
-
Plasmodium berghei
-
Stereoisomerism
-
Structure-Activity Relationship
-
Sulfides / chemical synthesis*
-
Sulfides / chemistry
-
Sulfides / therapeutic use
-
Sulfones / chemical synthesis
-
Sulfones / chemistry
-
Sulfones / therapeutic use
-
Sulfoxides / chemical synthesis
-
Sulfoxides / chemistry
-
Sulfoxides / therapeutic use
Substances
-
Anilides
-
Antimalarials
-
Sulfides
-
Sulfones
-
Sulfoxides
-
Mefloquine