Design and Synthesis of New N-(5-Trifluoromethyl)-1H-1,2,4-triazol-3-yl Benzenesulfonamides as Possible Antimalarial Prototypes
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-, 19F-NMR...
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2011-09-01
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Online Access: | http://www.mdpi.com/1420-3049/16/9/8083/ |
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doaj-a7b140427bd141c98e14489b620b29282020-11-24T22:25:16ZengMDPI AGMolecules1420-30492011-09-011698083809710.3390/molecules16098083Design and Synthesis of New N-(5-Trifluoromethyl)-1H-1,2,4-triazol-3-yl Benzenesulfonamides as Possible Antimalarial PrototypesNubia BoechatOsvaldo A. Santos-FilhoIsabor C. SilvaLuiz C.S. PinheiroA 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-, 19F-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.http://www.mdpi.com/1420-3049/16/9/8083/malariasulfonamidetrifluoromethyldihydropteroate synthaseDHPS |
collection |
DOAJ |
language |
English |
format |
Article |
sources |
DOAJ |
author |
Nubia Boechat Osvaldo A. Santos-Filho Isabor C. Silva Luiz C.S. Pinheiro |
spellingShingle |
Nubia Boechat Osvaldo A. Santos-Filho Isabor C. Silva Luiz C.S. Pinheiro Design and Synthesis of New N-(5-Trifluoromethyl)-1H-1,2,4-triazol-3-yl Benzenesulfonamides as Possible Antimalarial Prototypes Molecules malaria sulfonamide trifluoromethyl dihydropteroate synthase DHPS |
author_facet |
Nubia Boechat Osvaldo A. Santos-Filho Isabor C. Silva Luiz C.S. Pinheiro |
author_sort |
Nubia Boechat |
title |
Design and Synthesis of New N-(5-Trifluoromethyl)-1H-1,2,4-triazol-3-yl Benzenesulfonamides as Possible Antimalarial Prototypes |
title_short |
Design and Synthesis of New N-(5-Trifluoromethyl)-1H-1,2,4-triazol-3-yl Benzenesulfonamides as Possible Antimalarial Prototypes |
title_full |
Design and Synthesis of New N-(5-Trifluoromethyl)-1H-1,2,4-triazol-3-yl Benzenesulfonamides as Possible Antimalarial Prototypes |
title_fullStr |
Design and Synthesis of New N-(5-Trifluoromethyl)-1H-1,2,4-triazol-3-yl Benzenesulfonamides as Possible Antimalarial Prototypes |
title_full_unstemmed |
Design and Synthesis of New N-(5-Trifluoromethyl)-1H-1,2,4-triazol-3-yl Benzenesulfonamides as Possible Antimalarial Prototypes |
title_sort |
design and synthesis of new n-(5-trifluoromethyl)-1h-1,2,4-triazol-3-yl benzenesulfonamides as possible antimalarial prototypes |
publisher |
MDPI AG |
series |
Molecules |
issn |
1420-3049 |
publishDate |
2011-09-01 |
description |
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-, 19F-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. |
topic |
malaria sulfonamide trifluoromethyl dihydropteroate synthase DHPS |
url |
http://www.mdpi.com/1420-3049/16/9/8083/ |
work_keys_str_mv |
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