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

被引:61
作者
Boechat, Nubia [1 ]
Pinheiro, Luiz C. S. [1 ]
Santos-Filho, Osvaldo A. [1 ]
Silva, Isabor C. [1 ]
机构
[1] Fundacao Oswaldo Cruz, Dept Sintese Organ, Inst Tecnol Farmacos, BR-21041250 Rio De Janeiro, Brazil
关键词
malaria; sulfonamide; trifluoromethyl; dihydropteroate synthase; DHPS; CARBONIC-ANHYDRASE INHIBITORS; ORAL HYPOGLYCEMIC AGENTS; IN-VITRO; FLUORINE; DERIVATIVES; SULFONAMIDES; CHALCONE; SYNTHASE; SEARCH;
D O I
10.3390/molecules16098083
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
070307 [化学生物学]; 071010 [生物化学与分子生物学];
摘要
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.
引用
收藏
页码:8083 / 8097
页数:15
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