Portal de Periódicos da CAPES

Artigo Produção Nacional Revisado por pares

BIBTEX RIS

Design, Synthesis, and Trypanocidal Activity of Novel 5‐Nitroimidazolyl O ‐Benzyloxime Ethers

2017; Wiley; Volume: 54; Issue: 6 Linguagem: Inglês

10.1002/jhet.2989

1943-5193

Samir A. Carvalho, Luis Felipe Baumotte Osorio, Kelly Salomão, Solange L. de Castro, J.L. Wardell, J.L. Wardell, Edson Ferreira Da Silva, Carlos Alberto Manssour Fraga,

Research on Leishmaniasis Studies

In this paper, we describe the synthesis and the action against of the trypomastigote form of Trypanosoma cruzi of a new class of nitroimidazole‐2‐carbaldehyde O ‐benzyloximes. These derivatives were designed through the application of molecular hybridization concept between two potent antiprotozoal compounds, the 5‐nitrothiophene‐2‐carbaldehyde O ‐oxime 6 and the trypanocidal piperidinyl‐4‐carbaldehyde O ‐benzyloxime 7 with the intention of reaching two distinct molecular targets of T. cruzi . The activity of these benzyl ether derivatives was tested against the infective trypomastigote forms of T. cruzi , and the derivative ( E )‐1‐methyl‐5‐nitro‐1 H ‐imidazole‐2‐carbaldehyde O ‐(4‐nitrobenzyl) oxime ( 1 ) presented moderate trypanocidal activity (IC 50 = 12.7 μ M ) when compared with the standard drug benznidazole, which showed to be a good starting point for the design of more effective trypanocide agents.