A new class of antimalarial drugs: derivatives of benzothiopyrans.
A series of substituted benzothiopyrans was synthesized and examined for antimalarial activity. Some were found to be active and curative at dose levels of 160--360 mg/kg against Plasmodium berghei in mice. Afew observations concerning structure-activity relationships were made. The benzothiopyrans were prepared by treatment of either the gem-dichloro- or the thionothioflavone intermediate with various primary amines. The thionothioflavone intermediates were made from thioflavones. Condensation of thiophenols with benzoyl acetates gave the thioflavones.
D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000627:therapeutic use; D001578:Benzopyrans / Q000138:chemical synthesis* / Q000627:therapeutic use; D002645:Chickens; D008288:Malaria / Q000188:drug therapy; D051379:Mice; D010962:Plasmodium berghei; D013329:Structure-Activity Relationship
D000962:Antimalarials; D001578:Benzopyrans