Malaria-infected mice are completely cured by one 6 mg/kg oral dose of a new monomeric trioxane sulfide combined with mefloquine.

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.

• Authors: Rachel D Slack, Bryan T Mott, Lauren E Woodard, Abhai Tripathi, Abhai Triphati, David Sullivan, Elizabeth Nenortas, Sonya C T Girdwood, Theresa A Shapiro, Gary H Posner
• Journal: Journal of medicinal chemistry (J Med Chem) Vol. 55 Issue 1 Pg. 291-6 (Jan 12 2012) ISSN: 1520-4804 [Electronic] United States
• PMID: 22128829 (Publication Type: Journal Article, Research Support, N.I.H., Extramural, Research Support, Non-U.S. Gov't)

Chemical References

• Anilides
• Antimalarials
• Sulfides
• Sulfones
• Sulfoxides
• Mefloquine

Topics

• Administration, Oral
• Anilides (chemical synthesis, chemistry, therapeutic use)
• Animals
• Antimalarials (chemical synthesis, chemistry, therapeutic use)
• Drug Therapy, Combination
• Malaria (drug therapy)
• Mefloquine (therapeutic use)
• Mice
• Parasitemia (drug therapy)
• Plasmodium berghei
• Stereoisomerism
• Structure-Activity Relationship
• Sulfides (chemical synthesis, chemistry, therapeutic use)
• Sulfones (chemical synthesis, chemistry, therapeutic use)
• Sulfoxides (chemical synthesis, chemistry, therapeutic use)