Synthesis and Biological Evaluation of New Sulfonamide Derivatives as Potential Anti-Trypanosoma cruzi Agents

Author(s): Virgilio Bocanegra-Garcia, Juan Carlos Villalobos-Rocha, Benjamin Nogueda-Torres, Maria Edith Lemus- Hernandez, Argelia Camargo-Ordonez, Ninfa Maria Rosas-Garcia, Gildardo Rivera.

Journal Name: Medicinal Chemistry

Volume 8 , Issue 6 , 2012

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Chagas disease continues to be one of the main parasitic diseases in Latin America. Despite the fact that it was discovered more than 100 years ago, no suitable pharmacologic treatment is available. We report the synthesis of new sulfonamidoquinoline and sulfonamides derivatives that were evaluated in vitro against two strains of Trypanosoma cruzi (NINOA and INC-5). Structure-activity relationship analysis indicated that small aromatic and large aromatic substituents on 4-aminoquinaldine increased trypanocidal activity on INC-5 and NINOA strains, respectively. Additionally, results show the importance of the sulfonamide group as a scaffold for the development of new anti-T. cruzi agents. Seven sulfonamide derivatives showed better lytic activity than nifurtimox and beznidazole against both strains of T. cruzi. N- (biphenyl-4-yl-sulfonyl)-nicotinamide (P-012) was established as the leader of the series for the development of more effective agents.

Keywords: Biological Activity, Chagas, Synthesis, Sulfonamide, Sulfonamidoquinoline, Trypanosoma Cruzi

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Article Details

Year: 2012
Page: [1039 - 1044]
Pages: 6
DOI: 10.2174/1573406411208061039
Price: $58

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