Razdan R K, Bruni R J, Mehta A C, Weinhardt K K, Papanastassiou Z B
J Med Chem. 1978 Jul;21(7):643-9. doi: 10.1021/jm00205a010.
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.
