24590-06-5Relevant academic research and scientific papers
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.
Synthesis and metal ion complexation of acyclic Schiff base podands with lipophilic amide and ester end groups
Mizyed, Shehadeh,Ashram, Muhammad
scheme or table, p. 135 - 142 (2012/03/27)
A series of acyclic Schiff base podands 14-19 with lipophilic amide and ester end groups were synthesized in good yield and in a simple way. Their transition metal ions complexation was studied using conductometric method in acetonitrile (AN) at 25 °C. Schiff base podands 14-16 showed a continuous decrease in the molar conductances in their complexation with Hg2+, Pb2+, Cu2+, Zn2+ and Cd2+ which begins to level off at a mole ratio of 1:1 crown-to-metal indicating the formation of a stable 1:1 complexes. The order of the stability constants of the metal ions studied with the Schiff base podands 14, 15 and 16 is: Hg 2+ > Pb2+ > Cu2+ > Zn2+ > Cd2+ > Ag+. Metal ion complexation by acyclic diamide or diester podands involves presumably the oxygen atoms of the carbonyl groups in addition to the nitrogen atoms of the imino groups.
Discovery and optimisation of potent, selective, ethanolamine inhibitors of bacterial phenylalanyl tRNA synthetase
Jarvest, Richard L.,Erskine, Symon G.,Forrest, Andrew K.,Fosberry, Andrew P.,Hibbs, Martin J.,Jones, Joanna J.,O'Hanlon, Peter J.,Sheppard, Robert J.,Worby, Angela
, p. 2305 - 2309 (2007/10/03)
High throughput screening of Staphylococcus aureus phenylalanyl tRNA synthetase (FRS) identified ethanolamine 1 as a sub-micromolar hit. Optimisation studies led to the enantiospecific lead 64, a single-figure nanomolar inhibitor. The inhibitor series shows selectivity with respect to the mammalian enzyme and the potential for broad spectrum bacterial FRS inhibition.
