Abstract
An improved procedure for the synthesis of 3-amino-9-arylsubstituted-thieno[3,2- b]benzothiazine S, S-dioxide 2-decarboxylated is reported. Thieno-[3,2- b]benzothiazine S, S-dioxide derivatives were investigated for their abilities to inhibit β-hematin formation, hemoglobin hydrolysis and in vivo for their efficacy in rodent Plasmodium berghei. Compounds 5j– o were the most promising as inhibitors of hemoglobin hydrolysis, however, the compounds are not as efficient as chloroquine. A structure–activity relationship (SAR) study was carried out in this series. Our results allow us to determine the minimal structural requirements to produce the biological response.
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