8-(1-Naphthalen-2-yl-vinyl)-6,7,10-trioxaspiro (4.5) decane, a new 1,2,4-trioxane effective against rodent and simian malaria.
A new series of 8-(1-aryl-vinyl)-6,7,10-trioxaspiro [4.5] decanes 7a-e and 3-(1-aryl-vinyl)-l,2,5-trioxaspiro [5.5] undecanes 8a-e have been prepared and screened against multi-drug resistant Plasmodium yoelii in mice. 8-(1-Naphthalen-2-yl-vinyl)-6,7,10-trioxaspiro [4.5] decane 7b, the most active trioxane of the series, has also shown promising activity against Plasmodium cynomolgi in rhesus monkeys.
Singh
Chandan
C
Division of Medicinal and Process Chemistry, Central Drug Research Institute, Lucknow 226001, India. chandancdri@yahoo.com
Kanchan
Rani
R
Srivastava
Divya
D
Puri
Sunil K
SK
D000818:Animals; D000962:Antimalarials / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D018432:Drug Resistance, Multiple / Q000187:drug effects*; D000882:Haplorhini; D006571:Heterocyclic Compounds / Q000138:chemical synthesis / Q000494:pharmacology* / Q000627:therapeutic use; D008288:Malaria / Q000188:drug therapy; D051379:Mice; D009281:Naphthalenes / Q000138:chemical synthesis / Q000494:pharmacology*; D016789:Plasmodium cynomolgi / Q000187:drug effects*; D010967:Plasmodium yoelii / Q000187:drug effects*; D013141:Spiro Compounds / Q000138:chemical synthesis / Q000494:pharmacology*
C503429:1,2,4-trioxane; C508942:8-(1-naphthalen-2-yl-vinyl)-6,7,10-trioxaspiro (4.5) decane; D000962:Antimalarials; D006571:Heterocyclic Compounds; D009281:Naphthalenes; D013141:Spiro Compounds