Design and synthesis of new N-(5-trifluoromethyl)-1H-1,2,4-triazol-3-yl benzenesulfonamides as possible antimalarial prototypes |
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Authors: | Boechat Nubia Pinheiro Luiz C S Santos-Filho Osvaldo A Silva Isabor C |
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Institution: | Departamento de Sintese Organica, Instituto de Tecnologia em Farmacos, Fundacao Oswaldo Cruz, Manguinhos, CEP 21041-250, Rio de Janeiro, RJ, Brazil. boechat@far.fiocruz.br |
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Abstract: | A rational approach was used to synthesize a new set of 15 1H-1,2,4-triazol-3-yl benzenesulfonamide derivatives with the aim of developing new antimalarial lead compounds. These derivatives were prepared in yields between 50% and 62%, and their structures were elucidated using IR, 1H-, 13C-, 1?F-NMR, MS and elemental analysis. A docking study based on sulfonamides previously used against malaria identified trifluoromethyl-substituted derivatives to be the best lead compounds for new antimalarial drug development. |
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