Artículo
Salts of 5-amino-2-sulfonamide-1,3,4-thiadiazole, a structural and analog of acetazolamide, show interesting carbonic anhydrase inhibitory properties, diuretic, and anticonvulsant action
Diaz, Jorge R. A.; Camí, Gerardo Enrique; Liu González, Malva; Vega, Daniel Roberto; Vullo, Daniela; Juárez, Américo; Pedregosa, Jose Carmelo
; Supuran, Claudiu T.
Fecha de publicación:
10/2015
Editorial:
Taylor & Francis Ltd
Revista:
Journal of Enzyme Inhibition and Medicinal Chemistry
ISSN:
1475-6366
Idioma:
Inglés
Tipo de recurso:
Artículo publicado
Clasificación temática:
Resumen
Three salts of 5-amino-2-sulfonamide-1,3,4-thiadiazole (Hats) were prepared and characterized by physico-chemical methods. The p-toluensulfonate, the methylsulfonate, and the chlorhydrate monohydrate salts of Hats were evaluated as carbonic anhydrase (CA, EC 4.2.1.1) inhibitors (CAIs) and as anticonvulsants and diuretics, since many CAIs are clinically used as pharmacological agents. The three Hats salts exhibited diuretic and anticonvulsant activities with little neurotoxicity. The human (h) isoforms hCA I, II, IV, VII, IX, and XII were inhibited in their micromolar range by these salts, whereas pathogenic beta and gamma CAs showed similar, weak inhibitory profiles.
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Articulos(INTEQUI)
Articulos de INST. DE INVEST. EN TECNOLOGIA QUIMICA
Articulos de INST. DE INVEST. EN TECNOLOGIA QUIMICA
Citación
Diaz, Jorge R. A.; Camí, Gerardo Enrique; Liu González, Malva; Vega, Daniel Roberto; Vullo, Daniela; et al.; Salts of 5-amino-2-sulfonamide-1,3,4-thiadiazole, a structural and analog of acetazolamide, show interesting carbonic anhydrase inhibitory properties, diuretic, and anticonvulsant action; Taylor & Francis Ltd; Journal of Enzyme Inhibition and Medicinal Chemistry; 31; 6; 10-2015; 1102-1110
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