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Potential antichagasic compounds: design and synthesis of 1,2,4-triazolic bioisosteres of hydroxymethylnitrofurazone and analogues

Grant number: 12/21865-7
Support type:Scholarships in Brazil - Master
Effective date (Start): June 01, 2013
Effective date (End): August 31, 2014
Field of knowledge:Health Sciences - Pharmacy
Principal Investigator:Elizabeth Igne Ferreira
Grantee:Fredson Torres Silva
Home Institution: Faculdade de Ciências Farmacêuticas (FCF). Universidade de São Paulo (USP). São Paulo , SP, Brazil

Abstract

Chagas disease, parasitosis caused by Trypanosoma cruzi, is a disease that predominates in Latin America. It is estimated that 10 million people are under the risk of infection and, in 2008, more than 10 thousand deaths were registered. The only two drugs available in the therapeutics, nifurtimox and benznidazole, showed to be more effective in the acute phase of the disease. However, there is no choice for the chronic phase. Nitrofurazone (NF), an antimicrobial drug, has activity against T. cruzi, although being toxic. Its hydroxymethyl derivative, the hydroxymethylnitrofurazone (NFOH), showed to be more active and less toxic than the prototype. Considering the need for new antichagasic drugs, the existence of promising new therapeutic targets, as 14 alpha-sterol demethylase and cruzain, and by employing the bioisosterism approach, the purpose is to synthesize drug candidates as the 1,2,4-bioisosters of NFOH and analogs. We expect that the compounds obtained by this approach are more active and less toxic than the prototypes, due to the interaction of triazole ring nitrogen 1 with parasite 14 alpha-sterol demethylase.

Scientific publications
(References retrieved automatically from Web of Science and SciELO through information on FAPESP grants and their corresponding numbers as mentioned in the publications by the authors)
SILVA, FREDSON T.; FRANCO, CAIO H.; FAVARO, DENIZE C.; FREITAS-JUNIOR, LUCIO H.; MORAES, CAROLINA B.; FERREIRA, ELIZABETH I. Design, synthesis and antitrypanosomal activity of some nitrofurazone 1,2,4-triazolic bioisosteric analogues. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, v. 121, p. 553-560, OCT 4 2016. Web of Science Citations: 10.

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