126404-38-4Relevant academic research and scientific papers
Design, Synthesis, and Biological Evaluation of Itaconic Acid Derivatives as Potential Anti-Influenza Agents
Sethy, Bidyadhar,Hsieh, Chung-Fan,Lin, Ta-Jen,Hu, Po-Yuan,Chen, Yu-Li,Lin, Chia-Yi,Tseng, Sung-Nain,Horng, Jim-Tong,Hsieh, Pei-Wen
, p. 2390 - 2403 (2019)
Influenza A viruses (IAVs) have caused worldwide epidemics and pandemics by reassortment and generation of drug-resistant mutants, which render antivirals and current vaccinations no longer usable. In this study, an itaconic acid derivative 1 was identified from a chemical library of 20 000 compounds, by performing a cell-based screening assay, as a lead agent exhibiting anti-influenza A activity. Accordingly, a series of itaconic acid derivatives were designed and synthesized by adopting a rational design strategy to obtain more potent anti-influenza agents. The results of an in vitro pharmacological study showed that compounds 4 and 8 exhibited the most potent anti-IAV effect with half-maximal effective concentration values of 0.14 and 0.11 μM, respectively, in Madin-Darby canine kidney cells. The mechanism of action studies showed that lead agents 1 and 4 reduced virus replication by directly targeting IAV nucleoproteins and disrupting virus ribonucleoprotein export from the nucleus to the cytosol. On the basis of its high potential as an anti-IAV agent and its selectivity index >785, compound 4 was found to be a promising candidate for further development against IAVs.
SYNTHESIS AND BIOLOGICAL ACTIVITY OF SOME DERIVATIVES RELATED TO 2-METHYLENEBUTANEDIOIC ACID
Veverka, Miroslav,Kralovicova, Eva
, p. 2731 - 2737 (2007/10/02)
Nucleophilic reactions of methyl 3-chloroformyl-3-butenoate with N-substituted anilines and substituted phenols, and also preparation of 2-methylenebutanedioic acid monoanilides and their dehydration to the corresponding N-arylimides are described.
