861146-16-9Relevant academic research and scientific papers
Conjugation of N-acylhydrazone and 1,2,4-oxadiazole leads to the identification of active antimalarial agents
dos Santos Filho, José Maurício,de Queiroz e Silva, Diogo Manoel Alves,Macedo, Taís Soares,Teixeira, Helena Mariana Pitangueira,Moreira, Diogo Rodrigo Magalhaes,Challal, Soura,Wolfender, Jean-Luc,Queiroz, Emerson Ferreira,Soares, Milena Botelho Pereira
, p. 5693 - 5701 (2016/11/09)
Malaria, caused by several Plasmodium species, is the major life-threatening parasitic infection worldwide. Due to the parasite resistance to quinoline based drugs, the search for antimalarial agents is necessary. Here, we report the structural design, sy
Optimization of anti-Trypanosoma cruzi oxadiazoles leads to identification of compounds with efficacy in infected mice
Dos Santos Filho, Jose Mauricio,Moreira, Diogo Rodrigo M.,De Simone, Carlos Alberto,Ferreira, Rafaela Salgado,McKerrow, James H.,Meira, Cassio Santana,Guimaraes, Elisalva Teixeira,Soares, Milena Botelho Pereira
, p. 6423 - 6433,11 (2012/12/11)
We recently showed that oxadiazoles have anti-Trypanosoma cruzi activity at micromolar concentrations. These compounds are easy to synthesize and show a number of clear and interpretable structure-activity relationships (SAR), features that make them attr
NOVEL NK-3 RECEPTOR SELECTIVE ANTAGONIST COMPOUNDS, PHARMACEUTICAL COMPOSITION AND METHODS FOR USE IN NK-3 RECEPTORS MEDIATED DISORDERS
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Page/Page column 101-102, (2011/10/13)
The present invention is directed to novel compounds of formula I and their use as therapeutic compounds.
Design, synthesis and cruzain docking of 3-(4-substituted-aryl)-1,2,4-oxadiazole-N-acylhydrazones as anti-Trypanosoma cruzi agents
dos Santos Filho, Jose Mauricio,Leite, Ana Cristina Lima,Oliveira, Boaz Galdino de,Moreira, Diogo Rodrigo Magalhaes,Lima, Milena S.,Soares, Milena Botelho Pereira,Leite, Lucia Fernanda C.C.
scheme or table, p. 6682 - 6691 (2009/12/09)
Research in recent years has demonstrated that the Trypanosoma cruzi cysteine protease cruzain (TCC) is a valid chemotherapeutic target, since inhibitors of this protease affect the pathology appropriately. By exploring the N-acylhydrazones (NAH) as privi
Synthesis, biological evaluation, and structural studies of 3-phenyl[1,2,4]oxadiazole-5-carboxylic acid benzo[1,3]dioxol 5-ylmethylene-hydrazide
Santos-Filho,De Lima,Leite,Ximenes,Da Silva,Lima,Pitta
, p. 29 - 36 (2007/10/03)
A series of 1,2,4-oxadiazole combined with carbohydrazides residues, designed as possible bioactive compounds, was obtained in an attempt to analyse the effects of this molecular hybridization on the biological properties of the resulting compounds. They
