Design and Synthesis of New N-(5-Trifluoromethyl)-1H-1,2,4-triazol-3-yl Benzenesulfonamides as Possible Antimalarial Prototypes

作者：Boechat Nubia^*; Pinheiro Luiz C S; Santos Filho Osvaldo A; Silva Isabor C

来源：Molecules, 2011, 16(9): 8083-8097.

DOI：10.3390/molecules16098083

• malaria
• sulfonamide
• trifluoromethyl
• dihydropteroate synthase
• DHPS

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, H-1-, C-13-, F-19-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.

• 出版日期2011-9