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. © 2008 Elsevier Ltd. All rights reserved.
Original language | English |
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Pages (from-to) | 3661-3674 |
Journal | Bioorganic and Medicinal Chemistry |
Volume | 16 |
Issue number | 7 |
DOIs | |
Publication status | Published - 1 Apr 2008 |
Keywords
- 1,4-Benzothiazines
- Antimalarial
- Cyclization
- SAR study
- Thieno