TY - JOUR
T1 - Synthesis and biological evaluation of new sulfonamide derivatives as potential anti-Trypanosoma cruzi agents
AU - Bocanegra-Garcia, Virgilio
AU - Villalobos-Rocha, Juan Carlos
AU - Nogueda-Torres, Benjamín
AU - Lemus-Hernandez, María Edith
AU - Camargo-Ordoñez, Argelia
AU - Rosas-Garcia, Ninfa Maria
AU - Rivera, Gildardo
PY - 2012/11
Y1 - 2012/11
N2 - 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.
AB - 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.
KW - Biological Activity
KW - Chagas
KW - Sulfonamide
KW - Sulfonamidoquinoline
KW - Synthesis
KW - Trypanosoma Cruzi
UR - http://www.scopus.com/inward/record.url?scp=84868022288&partnerID=8YFLogxK
U2 - 10.2174/1573406411208061039
DO - 10.2174/1573406411208061039
M3 - Artículo
SN - 1573-4064
VL - 8
SP - 1039
EP - 1044
JO - Medicinal Chemistry
JF - Medicinal Chemistry
IS - 6
ER -