RT Journal Article
T1 Synthesis and Biological in vitro and in vivo Evaluation of 2-(5-Nitroindazol-1-yl)ethylamines and Related Compounds as Potential Therapeutic Alternatives for Chagas Disease.
A1 Martín-Escolano, Rubén
A1 Aguilera-Venegas, Benjamín
A1 Marín, Clotilde
A1 Martín-Montes, Álvaro
A1 Martín-Escolano, Javier
A1 Medina-Carmona, Encarnación
A1 Arán, Vicente J
A1 Sánchez-Moreno, Manuel
K1 Chagas disease
K1 Trypanosoma cruzi
K1 antiprotozoal agents
K1 drug discovery
K1 nitroheterocycles
AB Chagas disease, a neglected tropical disease caused by infection with the protozoan parasite Trypanosoma cruzi, is a potentially life-threatening illness that affects 5-8 million people in Latin America, and more than 10 million people worldwide. It is characterized by an acute phase, which is partly resolved by the immune system, but then develops as a chronic disease without an effective treatment. There is an urgent need for new antiprotozoal agents, as the current standard therapeutic options based on benznidazole and nifurtimox are characterized by limited efficacy, toxicity, and frequent failures in treatment. In vitro and in vivo assays were used to identify some new low-cost 5-nitroindazoles as a potential antichagasic therapeutic alternative. Compound 16 (3-benzyloxy-5-nitro-1-vinyl-1H-indazole) showed improved efficiency and lower toxicity than benznidazole in both in vitro and in vivo experiments, and its trypanocidal activity seems to be related to its effect at the mitochondrial level. Therefore, compound 16 is a promising candidate for the development of a new anti-Chagas agent, and further preclinical evaluation should be considered.
YR 2018
FD 2018-09-04
LK http://hdl.handle.net/10668/12822
UL http://hdl.handle.net/10668/12822
LA en
DS RISalud
RD Apr 4, 2025