New orally active spiro 1,2,4-trioxanes with high antimalarial potency.
A new series of functionalized 1,2,4-trioxanes 10-21 have been prepared and assessed for antimalarial activity in mice. Several of these trioxanes show significant activity. Trioxane 16, the most active compound of the series, has shown activity by oral route which is comparable with that of the clinically used drug, beta-arteether.
Singh
Chandan
C
Division of Medicinal and Process Chemistry, Central Drug Research Institute, Lucknow 226001, India. chandancdri@yahoo.com
Malik
Heetika
H
Puri
Sunil K
SK
D000284:Administration, Oral; D000818:Animals; D000962:Antimalarials / Q000008:administration & dosage / Q000494:pharmacology*; D004351:Drug Resistance; D006571:Heterocyclic Compounds / Q000008:administration & dosage / Q000494:pharmacology*; D051379:Mice; D010967:Plasmodium yoelii / Q000187:drug effects
C503429:1,2,4-trioxane; D000962:Antimalarials; D006571:Heterocyclic Compounds