65654-29-7Relevant academic research and scientific papers
Synthesis and preliminary anti-inflammatory and anti-bacterial evaluation of some diflunisal aza-analogs
Carta, Davide,Brun, Paola,Dal Pra, Matteo,Bernabè, Giulia,Castagliuolo, Ignazio,Ferlin, Maria Grazia
, p. 1017 - 1032 (2018/06/27)
Our aim was to identify new multi-target compounds endowed with both anti-inflammatory and anti-bacterial activities for treatment of human infections. Diflunisal, a nonsteroidal anti-inflammatory agent, has recently been repurposed for its anti-virulence properties against methicillin-resistant Staphylococcus aureus. Effective synthesis of some aza-analogs of the anti-inflammatory drug diflunisal was carried out following the route involving key oxazole intermediates to obtain o- and m-hydroxypyridinecarboxylic acid derivatives. The newly synthesized diflunisal aza-analogs did not exhibit cytotoxic activity up to 80 μM and some of them exhibited anti-inflammatory activities, decreasing the levels of pro-inflammatory cytokines and prostaglandins induced by bacterial lipopolysaccharide in human primary macrophages. Ten of the diflunisal aza-analogs were found to have interesting antibacterial activity, sensitizing S. aureus, Streptococcus pyogenes, Enterococcus faecium, and Pseudomonas aeruginosa to the antibacterial effects of beta-lactam antibiotics and protein synthesis inhibitors.
Copper-Catalyzed Aerobic Oxidative [2 + 3] Cyclization/Aromatization Cascade Reaction: Atom-Economical Access to Tetrasubstituted 4,5-Biscarbonyl Imidazoles
Xie, Jialin,Huang, Yuanqiong,Song, Hongjian,Liu, Yuxiu,Wang, Qingmin
supporting information, p. 6056 - 6059 (2017/11/27)
An atom-economical method for accessing tetrasubstituted 4,5-biscarbonylimidazoles by reaction between glycine derivatives and 5-alkoxyoxazoles is reported. The method, which involves a copper-catalyzed aerobic oxidative [2 + 3] cyclization/aromatization
Benzyl [11C]Hippurate as an Agent for Measuring the Activities of Organic Anion Transporter 3 in the Brain and Multidrug Resistance-Associated Protein 4 in the Heart of Mice
Kikuchi, Tatsuya,Okamura, Toshimitsu,Okada, Maki,Ogawa, Masanao,Suzuki, Chie,Wakizaka, Hidekatsu,Yui, Joji,Fukumura, Toshimitsu,Gee, Antony D.,Zhang, Ming-Rong
, p. 5847 - 5856 (2016/07/06)
Multidrug resistance-associated protein 4 (MRP4) and organic anion transporter 3 (OAT3) mediate the efflux of organic anions from the brain and heart. In this study, we have developed a probe for estimating the activity of these transporters in these tiss
A NEW PATHWAY TO 1,3,4(2H)-ISOQUINOLINETRIONES AND SUBSTITUTED ISOINDOLINONES
Vekemans, Jozef,Hoornaert, Georges
, p. 943 - 950 (2007/10/02)
A new synthesis in the isoquinoline series is discussed: the reaction of appropriate benzamides and oxalyl chloride affords isoquinolinetrions along N-aroyloxamoyl chlorides.The solvent effect, the acid catalysis and the isomer distribution are accounted
