Advanced search
Start date
Betweenand
Related content
(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

Pyrazinoates as antiparasitic agents against Trypanosoma cruzi

Full text
Author(s):
Vasconcelos, Camilla I. [1] ; Varela, Marina T. [1] ; Torrecilhas, Ana C. [1] ; Fernandes, Joao P. S. [1]
Total Authors: 4
Affiliation:
[1] Univ Fed Sao Paulo, Dept Ciencias Farmaceut, Rua Sao Nicolau 210, BR-09913030 Diadema, SP - Brazil
Total Affiliations: 1
Document type: Journal article
Source: ARCHIV DER PHARMAZIE; v. 351, n. 11 NOV 2018.
Web of Science Citations: 0
Abstract

This work reports a repurposing study of pyrazinoic acid (1) and methyl (2), ethyl (3) and 2-chloroethyl (4) ester derivatives with antimycobacterial activity, in assays against Trypanosoma cruzi. The compounds and benznidazole, the standard antitrypanosoma drug, were evaluated in concentrations ranging from 100 to 6.25 mu g/mL. The results showed that compounds 2 and 3 (EC50 = 182 and 447 mu M) significantly reduced the infection rate of the parasite into the mammalian cells at 100 mu g/mL (p < 0.05) in a similar way to benznidazole. In addition, all the compounds also significantly reduced the number of intracellular parasites (compound 1 at 50 mu g/mL, and compounds 2-4 at 100 mu g/mL, p < 0.05) in comparison to the control. Compounds 1 and 2 were more effective than benznidazole at 50 mu g/mL (p < 0.001). Moreover, compounds 1-4 did not show significant cytotoxicity against THP-1, J774, and HeLa cells (>1000 mu M), indicating that they possess considerable selectivity against the parasites. This report represents the first study of such compounds against T. cruzi, indicating the potential of pyrazinoates as antiparasitic agents. (AU)

FAPESP's process: 16/01917-3 - The immunomodulatory role of extracellular vesicles shedding from infected macrophages by the Trypanosoma cruzi.
Grantee:Ana Claudia Trocoli Torrecilhas
Support Opportunities: Regular Research Grants
FAPESP's process: 18/03918-2 - Evaluation of the antiparasitic activity and cytotoxicity of natural products derivatives in Trypanosoma cruzi: design and synthesis of analogues potentially superior
Grantee:Marina Themoteo Varela
Support Opportunities: Scholarships in Brazil - Doctorate
FAPESP's process: 16/25028-3 - Antihistamines H3R/H4R as procognitive agents: a multitarget approach
Grantee:João Paulo dos Santos Fernandes
Support Opportunities: Regular Research Grants