Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 57, Issue 3, Pages 987-999Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm4017015
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Funding
- Spanish Ministry of Economy and Competitiveness (MINECO) [CTQ2011-27512/BQU, CSD2010-00065]
- Direccio General de Recerca, Desenvolupament Tecnologic i Innovacio del Govern Balear (CAIB) [23/2011]
- Ministry of Education of Spain
- FEDER
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Access to basic drugs is a major issue in developing countries. Chagas disease caused by Trypanosorna 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 Lipiriski's rule of five compliant squararnides 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.
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