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Molecules 2011, 16(9), 8083-8097; doi:10.3390/molecules16098083

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

Departamento de Sintese Organica, Instituto de Tecnologia em Farmacos, Fundacao Oswaldo Cruz, Manguinhos, CEP 21041-250, Rio de Janeiro, RJ, Brazil
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Received: 1 August 2011 / Revised: 9 September 2011 / Accepted: 16 September 2011 / Published: 20 September 2011
(This article belongs to the Special Issue Fluorine Chemistry 2016)
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Abstract

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.
Keywords: malaria; sulfonamide; trifluoromethyl; dihydropteroate synthase; DHPS malaria; sulfonamide; trifluoromethyl; dihydropteroate synthase; DHPS
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MDPI and ACS Style

Boechat, N.; Pinheiro, L.C.; Santos-Filho, O.A.; Silva, I.C. Design and Synthesis of New N-(5-Trifluoromethyl)-1H-1,2,4-triazol-3-yl Benzenesulfonamides as Possible Antimalarial Prototypes. Molecules 2011, 16, 8083-8097.

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