Evaluation of the Parasiticidal Activity of New 3-Nitro-1H-1,2,4-Triazole Analogues Encapsulated in Nanostructures

• Grant number: 24/19066-6
• Support Opportunities: Scholarships in Brazil - Scientific Initiation
• Start date: January 01, 2025
• End date: December 31, 2025
• Field of knowledge: Health Sciences - Pharmacy - Medicines Analysis and Control
• Principal Investigator: Sérgio de Albuquerque
• Grantee: João Henrique Stempkoski da Rosa
• Host Institution: Faculdade de Ciências Farmacêuticas de Ribeirão Preto (FCFRP). Universidade de São Paulo (USP). Ribeirão Preto , SP, Brazil

Abstract

Chagas disease is a Neglected Tropical Disease (NTD) that affects 6 million people worldwide, with an incidence of 12,000 deaths annually. In addition to underreporting, the available treatments (benznidazole and nifurtimox) show low efficacy in the chronic phase of the disease, encouraging the search for new therapeutic schemes. Microemulsions are viable strategies for this, considering the possible increase in drug bioavailability in these systems. With this in mind, Pelizaro et al. (2024) developed 2 analogues of 3-nitro-1H-1,2,4-triazole that showed potent in vitro biological activity against the Tulahuen strain of Trypanosoma cruzi in LLC-MK2 cell lines. Compound A showed an IC50 of 0.31±0.06 µmol.L-1 (SI >555) accompanied by 0.31±0.06 µmol.L-1 (SI >161) for B. This project proposes the nano-structuring of these compounds in microemulsions, using GTCC as the oil phase and Kholliphor® as the surfactant, to evaluate the alteration of in vitro biological activity against T. cruzi.