Synthesis and antimalarial activity of 6-cycloalkylvinyl substituted 1,2,4-trioxanes.
6-Cycloalkylvinyl substituted 1,2,4-trioxanes 6-15 have been prepared and tested against multi-drug resistant Plasmodium yoelii in mice. The most active trioxane 11 provides 80% protection to the treated mice. Further derivatization of 11 leads to decrease in antimalarial activity.
Singh
Chandan
C
Division of Medicinal and Process Chemistry, Central Drug Research Institute, Lucknow 226001, India. chandancdri@yahoo.com
Srivastav
Naveen Chandra
NC
Puri
Sunil K
SK
D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000494:pharmacology; D003516:Cycloparaffins / Q000138:chemical synthesis* / Q000494:pharmacology; D004852:Epoxy Compounds / Q000138:chemical synthesis / Q000494:pharmacology; D051379:Mice; D010967:Plasmodium yoelii / Q000187:drug effects* / Q000254:growth & development; D014753:Vinyl Compounds / Q000138:chemical synthesis* / Q000494:pharmacology
D000962:Antimalarials; D003516:Cycloparaffins; D004852:Epoxy Compounds; D014753:Vinyl Compounds; C012469:oxirene