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

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

Volume: 8 Issue: 6

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

Affiliation:

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

Abstract: 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.

Cite this article as:

Bocanegra-Garcia Virgilio, Carlos Villalobos-Rocha Juan, Nogueda-Torres Benjamin, Edith Lemus- Hernandez Maria, Camargo-Ordonez Argelia, Maria Rosas-Garcia Ninfa and Rivera Gildardo, Synthesis and Biological Evaluation of New Sulfonamide Derivatives as Potential Anti-Trypanosoma cruzi Agents, Medicinal Chemistry 2012; 8 (6) . https://dx.doi.org/10.2174/1573406411208061039