Orally active amino functionalized antimalarial 1,2,4-trioxanes.
Using readily available trioxanes 6a-b, a new series of amino functionalized 1,2,4-trioxanes 8a-e and 9a-e have been prepared and evaluated for antimalarial activity against multi-drug resistant Plasmodium yoelii in Swiss mice model. Several of these novel trioxanes are orally more active than the parent trioxanes 6a-b. Antimalarial activity of amino functionalized trioxane 9a, the most potent compound in the series, is very close to that of beta-arteether.
Singh
Chandan
C
Division of Medicinal Chemistry, Central Drug Research Institute, -226001, Lucknow, India. chandancdri@yahoo.com
Malik
Heetika
H
Puri
Sunil K
SK
D000284:Administration, Oral; D000818:Animals; D000962:Antimalarials / Q000008:administration & dosage* / Q000138:chemical synthesis*; D018432:Drug Resistance, Multiple / Q000187:drug effects / Q000502:physiology; D008288:Malaria / Q000097:blood / Q000188:drug therapy; D051379:Mice; D010967:Plasmodium yoelii / Q000187:drug effects* / Q000254:growth & development / Q000378:metabolism
D000962:Antimalarials