Synthesis and antimalarial activity of a new series of trioxaquines.
Trioxanes 8a-b, easily accessible in two steps from allylic alcohol 6a-b, on reductive amination with 4-aminoquinolines 4a-c furnish a new series of trioxaquines 9a-b, 10a-b, 11a-b in 32-77% yields. Dicitrate salts of these trioxaquines have been evaluated for antimalarial activity against multidrug resistant Plasmodium yoelii in mice model.
Division of Medicinal Chemistry, Central Drug Research Institute, Lucknow-226001, India. chandancdri@yahoo.com
Chandan
C
Singh
Heetika
H
Malik
Sunil K
SK
Puri
D000634:Aminoquinolines / Q000138:chemical synthesis* / Q000494:pharmacology*; D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000494:pharmacology; D001713:Biphenyl Compounds / Q000138:chemical synthesis* / Q000494:pharmacology*; D018432:Drug Resistance, Multiple; D008288:Malaria / Q000188:drug therapy; D051379:Mice; D010967:Plasmodium yoelii / Q000187:drug effects; D011804:Quinolines / Q000138:chemical synthesis* / Q000494:pharmacology*; D013141:Spiro Compounds / Q000138:chemical synthesis* / Q000494:pharmacology*; D015996:Survival Rate
D000634:Aminoquinolines; D000962:Antimalarials; D001713:Biphenyl Compounds; D011804:Quinolines; D013141:Spiro Compounds