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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Main Authors: Nubia Boechat, Osvaldo A. Santos-Filho, Isabor C. Silva, Luiz C.S. Pinheiro
Format: Article
Language:English
Published: MDPI AG 2011-09-01
Series:Molecules
Subjects:
Online Access:http://www.mdpi.com/1420-3049/16/9/8083/
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spelling 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/
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