119787-86-9Relevant academic research and scientific papers
Synthesis of Oxindole Derivatives via Intramolecular C–H Insertion of Diazoamides Using Ru(II)-Pheox Catalyst
Phan Thi Thanh, Nga,Dang Thi Thu, Huong,Tone, Masaya,Inoue, Hayato,Iwasa, Seiji
, (2020/10/02)
This work presented the efficient intramolecular aromatic C–H insertion of diazoacetamide. The 1a–1o diazo compounds (except for 1k) were converted into their corresponding oxindoles via an intramolecular C–H insertion reaction in the presence of a Ru catalyst. The Ru-Pheox catalyst was shown to be highly efficient in this transformation in terms of the regioselectivity, producing the desired products in excellent yield (99%). The efficiency of the Ru catalyst reached 580 (TON) and 156 min?1 (TOF).
New insights into the SAR and drug combination synergy of 2-(quinolin-4-yloxy)acetamides against Mycobacterium tuberculosis
Giacobbo, Bruno Couto,Pissinate, Kenia,Rodrigues-Junior, Valnês,Villela, Anne Drumond,Grams, Estêv?o Silveira,Abbadi, Bruno Lopes,Subtil, Fernanda Teixeira,Sperotto, Nathalia,Trindade, Rogério Valim,Back, Davi Fernando,Campos, Maria Martha,Basso, Luiz Augusto,Machado, Pablo,Santos, Diógenes Santiago
supporting information, p. 491 - 501 (2016/12/09)
2-(Quinolin-4-yloxy)acetamides have been described as potent and selective in vitro inhibitors of Mycobacterium tuberculosis (Mtb) growth. Herein, a new series of optimized compounds were found to demonstrate highly potent antitubercular activity, with minimum inhibitory concentration (MIC) values against drug-susceptible and drug-resistant Mycobacterium tuberculosis strains in the submicromolar range. Furthermore, the most active compounds had no apparent toxicity to mammalian cells, and they showed intracellular activities similar to those of isoniazid and rifampin in a macrophage model of Mtb infection. Use of the checkerboard method to investigate the association profiles of lead compounds with first- and second-line antituberculosis drugs showed that 2-(quinolin-4-yloxy)acetamides have a synergistic effect with rifampin. Ultimately, the good permeability, moderate rates of metabolism and low risk of drug-drug interactions displayed by some of the synthesized compounds indicate that 2-(quinolin-4-yloxy)acetamides may yield candidates to use in the development of novel alternative therapeutics for tuberculosis treatment.
Synthesis of phenoxyacetic acid derivatives as highly potent antagonists of gastrin/cholecystokinin-B receptors. II
Takeda, Yasuyuki,Kawagoe, Keiichi,Yokomizo, Aki,Yokomizo, Yoshihiro,Hosokami, Toru,Shimoto, Yoshimasa,Tabuchi, Yoshiaki,Ogihara, Yoshiyasu,Otsubo, Rira,Honda, Yuko,Yokohama, Shuichi
, p. 951 - 961 (2007/10/03)
A series of phenoxyacetanilide derivatives was synthesized and their antagonist activities for human gastrin/cholecystokinin (CCK)-B and CCK-A receptors were evaluated. Among the compounds synthesized, 2-[3-[3-[N-[2-(N- methyl-N-phenylcarbamoylmethoxy)phe
Cycloadditions, 15. - Influence of Substituents in p-, m-, and o-Position of the Arene onto the Intramolecular Diels-Alder Reaction of Allenecarboxylic Acid Anilides and Phenyl Esters
Himbert, Gerhard,Fink, Dieter,Diehl, Klaus,Rademacher, Paul,Bittner, Andreas J.
, p. 1161 - 1174 (2007/10/02)
The ylides 3 and 8 (synthesized via the bromoacetic acid amides 1 and -esters 6 and via the phosphonium bromides 2 and 7) react with ketene to give the allenecarboxanilides 4 and the phenyl allenecarboxylates 9.Thermolysis in boiling xylene of all derivat
