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

被引：50
|
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
来源：
MOLECULES | 2011年 / 16卷 / 09期
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：
071010 ; 081704 ;
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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