6-(4'-Aryloxy-phenyl)vinyl-1,2,4-trioxanes: a new series of orally active peroxides effective against multidrug-resistant Plasmodium yoelii in Swiss mice.
A new series of 6-(4'-aryloxy-phenyl)vinyl-1,2,4-trioxanes 10a-d, 11a-d, and 12a-d have been synthesized and evaluated for their antimalarial activity against multidrug-resistant Plasmodium yoelii in Swiss mice by oral route. Trioxanes 10b and 10c, the two most active compounds of the series, provided 100% protection to the infected mice at 48 mg/kg x 4 days. Clinically useful drug beta-arteether provided 100% and 20% protection at 48 mg/kg x 4 days and 24 mg/kg x 4 days, respectively, in this model.
Singh
Chandan
C
Division of Medicinal and Process Chemistry, Central Drug Research Institute, Lucknow, India. chandancdri@yahoo.com
Verma
Ved Prakash
VP
Naikade
Niraj Krishna
NK
Singh
Ajit Shankar
AS
Hassam
Mohammad
M
Puri
Sunil K
SK
D000284:Administration, Oral; D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D018432:Drug Resistance, Multiple; D006571:Heterocyclic Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D051379:Mice; D010967:Plasmodium yoelii / Q000187:drug effects*; D013329:Structure-Activity Relationship; D014753:Vinyl Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology
C503429:1,2,4-trioxane; D000962:Antimalarials; D006571:Heterocyclic Compounds; D014753:Vinyl Compounds