Synthesis, antimalarial activity, structure-activity relationship analysis of thieno-(3,2-b)benzothiazine S,S-dioxide analogs.

Barazarte A; Camacho J; Dominguez JLobo GGamboa NRodrigues JCapparelli MVAlvarez-Larena AAndujar SEnriz DCharris J

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Synthesis, antimalarial activity, structure-activity relationship analysis of thieno-(3,2-b)benzothiazine S,S-dioxide analogs.

机译：Synthesis, antimalarial activity, structure-activity relationship analysis of thieno-(3,2-b)benzothiazine S,S-dioxide analogs.

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An improved procedure for the synthesis of 3-amino-9-arylsubstituted-thieno3,2-bbenzothiazine S,S-dioxide 2-decarboxylated is reported. Thieno-3,2-bbenzothiazine S,S-dioxide derivatives were investigated for their abilities to inhibit beta-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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《Bioorganic and medicinal chemistry》 |2008年第7期|3661-3674|共14页
作者
Barazarte A; Camacho J; Dominguez JLobo GGamboa NRodrigues JCapparelli MVAlvarez-Larena AAndujar SEnriz DCharris J;
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作者单位

Laboratorio de Sintesis Organica, Universidad Central de Venezuela, Apartado 47206, Los Chaguaramos, 1041-A Caracas, Venezuela.;

ost.saga-med.ac.jp;

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正文语种英语
中图分类药学;生物化学;
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Animals; Antimalarials; Benzene; Crystallography; X-Ray; Electrostatics; 动物; 抗疟药; 苯; 结晶学; X线; 静电学; 血红素蛋白类; 小鼠; 模型; 分子; 分子结构;

Synthesis, antimalarial activity, structure-activity relationship analysis of thieno-(3,2-b)benzothiazine S,S-dioxide analogs.

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