99698-69-8Relevant academic research and scientific papers
Diversity-oriented synthesis of pyrazoles derivatives from flavones and isoflavones leads to the discovery of promising reversal agents of fluconazole resistance in Candida albicans
Cui, Chang-Yi,Liu, Jun,Zheng, Hong-Bo,Jin, Xue-Yang,Zhao, Xiao-Yu,Chang, Wen-Qiang,Sun, Bin,Lou, Hong-Xiang
, p. 1545 - 1549 (2018)
Diversity-oriented synthesis of derivatives of natural products is an important approach for the discovery of novel drugs. In this paper, a series of novel 3,4-diaryl-1H-pyrazoles and 3,5-diaryl-1H-pyrazoles derivatives were synthesized through the one-po
Synthesis and anti-trypanosoma cruzi activity of diaryldiazepines
Menezes, Jlio Csar L.,Vaz, Luana Beatriz A.,De Vieira, Paula Melo Abreu,Fonseca, Ktia Da Silva,Carneiro, Cludia Martins,Taylor, Jason G.
, p. 43 - 51 (2015/01/30)
Chagas disease is a so-called "neglected disease" and endemic to Latin America. Nifurtimox and benznidazole are drugs that have considerable efficacy in the treatment of the acute phase of the disease but cause many significant side effects. Furthermore, in the Chronic Phase its efficiency is reduced and their therapeutic effectiveness is dependent on the type of T. cruzi strain. For this reason, the present work aims to drive basic research towards the discovery of new chemical entities to treat Chagas disease. Differently substituted 5,7-diaryl-2,3-dihydro-1,4-diazepines were synthesized by cyclocondensation of substituted flavones with ethylenediamine and tested as anti-Trypanosoma cruzi candidates. Epimastigotes of the Y strain from T. cruzi were used in this study and the number of parasites was determined in a Neubauer chamber. The most potent diaryldiazepine that reduced epimastigote proliferation exhibited an IC50 value of 0.25 μM, which is significantly more active than benznidazole.
