A new class of antimalarial drugs: Derivatives of benzothiopyrans

Article abstract of 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. A few 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.