30893-64-2Relevant academic research and scientific papers
A phenoxy acetyl amine compound preparation method and phenoxy acetamide compounds
-
Paragraph 0040; 0041; 0047; 0048; 0049-0053, (2019/05/21)
The invention belongs to the organic intermediates and the technical field of pharmaceutical intermediates, in particular to a phenoxy acetyl amine compound preparation method and phenoxy acetyl amine compound. The present invention provides a preparation method of the pervasive should be good, and green environmental protection, has better popularization and application value. The results show that the embodiment, the invention provides the above-mentioned method can prepare a plurality of phenoxy acetyl amine compound, and the yield can be 76%.
Synthesis and biological evaluation of 2-Phenoxyacetamide analogues, a novel class of potent and selective monoamine oxidase inhibitors
Shen, Wei,Yu, Shian,Zhang, Jiaming,Jia, Weizheng,Zhu, Qing
, p. 18620 - 18631 (2015/01/08)
Monoamine oxidases (EC 1.4.3.4; MAOs), a family of FAD-containing enzymes, is an important target for antidepressant drugs. In this paper, a series of 2-phenoxyacetamide analogues were synthesized, and their inhibitory potency towards monoamine oxidases A (MAO-A) and B (MAO-B) were evaluated using enzyme and cancer cell lysate. 2-(4-Methoxyphenoxy)acetamide (compound 12) (SI = 245) and (2-(4-((prop-2- ynylimino)methyl)phenoxy)acetamide (compound 21) (IC50MAO-A = 0.018 μM, IC50MAO-B = 0.07 μM) were successfully identified as the most specific MAO-A inhibitor, and the most potent MAO-A/-B inhibitor, respectively. The inhibitory activities of these two compounds in living cells were also further evaluated utilizing HepG2 and SHSY-5Y cell lysates.
Discovery of a new series of 5-HT1A receptor agonists
Franchini, Silvia,Prandi, Adolfo,Sorbi, Claudia,Tait, Annalisa,Baraldi, Annamaria,Angeli, Piero,Buccioni, Michela,Cilia, Antonio,Poggesi, Elena,Fossa, Paola,Brasili, Livio
scheme or table, p. 2017 - 2020 (2010/07/07)
Starting from compounds previously identified as α1-adrenoceptor antagonists that were also found to bind to the 5-HT1A receptor, in an attempt to separate the two activities, a new series of 5-HT1A receptor agonists was identified and shown to have high potency and/or high selectivity. Of these, compound 13, which combines high selectivity (5-HT1A/α1 = 151) and good agonist potency (pD2 = 7.82; Emax = 76), was found to be the most interesting.
Efficient method for the direct preparation of amides from carboxylic acids using tosyl chloride under solvent-free conditions
Khalafi-Nezhad, Ali,Parhami, Abolfath,Soltani Rad, Mohammad Navid,Zarea, Abdolkarim
, p. 6879 - 6882 (2007/10/03)
A simple, clean and highly efficient solvent-free procedure for the preparation of primary, secondary, tertiary and aromatic amides is described from the direct reaction of carboxylic acids and silica-supported ammonium salts, triethylamine (TEA) and tosyl chloride (TsCl) as condensing agent. The reaction proceeds rapidly in high yields at room temperature.
