- A phenoxy acetyl amine compound preparation method and phenoxy acetamide compounds
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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%.
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Paragraph 0040; 0041; 0047; 0048; 0049-0053
(2019/05/21)
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- Synthesis and biological evaluation of 2-Phenoxyacetamide analogues, a novel class of potent and selective monoamine oxidase inhibitors
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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.
- Shen, Wei,Yu, Shian,Zhang, Jiaming,Jia, Weizheng,Zhu, Qing
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p. 18620 - 18631
(2015/01/08)
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