@misc{10481/101075,
year = {2014},
url = {https://hdl.handle.net/10481/101075},
abstract = {Access to basic drugs is a major issue in developing countries. Chagas disease caused by Trypanosoma cruzi is a paradigmatic example of a chronic disease without an effective treatment. Current treatments based on benznidazole and nifurtimox are expensive, ineffective, and toxic. N,N'-Squaramides are amide-type compounds that feature both hydrogen bond donor and acceptor groups and are capable of multiple interactions with complementary sites. When combined with amine and carboxylic groups, squaramide compounds have increased solubility and therefore make suitable therapeutic agents. In this work, we introduce a group of Lipinski's rule of five compliant squaramides as candidates for treating Chagas disease. The in vivo studies confirmed the positive expectations arising from the preliminary in vitro studies, revealing compound 17 to be the most effective for both acute and chronic phases. The activity, stability, low cost of starting materials, and straightforward synthesis make amino squaramides appropriate molecules for the development of an affordable anti-Chagasic agent.},
organization = {Spanish Ministry of Economy and Competitiveness (MINECO) (CTQ2011-27512/BQU; CONSOLIDER-INGENIO 2010 CSD2010-00065, FEDER funds);  "Direcció General de Recerca, Desenvolupament Tecnològic i Innovació del Govern Balear" (CAIB, project 23/2011, FEDER funds)},
title = {Synthesis and biological evaluation of N,N'-squaramides with high in vivo efficacy and low toxicity: toward a low-cost drug against Chagas disease},
doi = {10.1021/jm4017015},
author = {Olmo, Francisco and Rotger, Carmen and Ramírez-Macías, Inmaculada and Martínez, Luis and Marín Sánchez, Clotilde and Carreras, Lucas and Urbanová, Kristína and Vega, Manel and Chaves-Lemaur, Guillermo and Sampedro, Angel and Rosales Lombardo, María José and Sánchez Moreno, Manuel and Costa, Antonio},
}