Artículo
Synthesis, antimalarial activity, structure–activity relationship analysis of thieno-[3,2-b]benzothiazine S,S-dioxide analogs
Barazarte, Arthur; Camacho, José; Domínguez, José; Lobo, Gricela; Gamboa, Neira; Rodrigues, Juan; Capparelli, Mario V.; Álvarez Larena, Ángel; Andujar, Sebastian Antonio
; Enriz, Ricardo Daniel
; Charris, Jaime
Fecha de publicación:
04/2008
Editorial:
Pergamon-Elsevier Science Ltd
Revista:
Bioorganic & Medicinal Chemistry
ISSN:
0968-0896
Idioma:
Inglés
Tipo de recurso:
Artículo publicado
Clasificación temática:
Resumen
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.
Palabras clave:
1,4-BENZOTHIAZINES
,
ANTIMALARIAL
,
CYCLIZATION
,
SAR STUDY
,
THIENO
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Articulos(IMIBIO-SL)
Articulos de INST. MULTIDICIPLINARIO DE INV. BIO. DE SAN LUIS
Articulos de INST. MULTIDICIPLINARIO DE INV. BIO. DE SAN LUIS
Citación
Barazarte, Arthur; Camacho, José; Domínguez, José; Lobo, Gricela; Gamboa, Neira; et al.; Synthesis, antimalarial activity, structure–activity relationship analysis of thieno-[3,2-b]benzothiazine S,S-dioxide analogs; Pergamon-Elsevier Science Ltd; Bioorganic & Medicinal Chemistry; 16; 7; 4-2008; 3661-3674
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