《Novel fused pyridine derivatives containing pyrimidine moiety as prospective tyrosyl-tRNA synthetase inhibitors: Design, synthesis, pharmacokinetics and molecular docking studies》 was written by Othman, Ismail M. M.; Gad-Elkareem, Mohamed A. M.; Anouar, El Hassane; Snoussi, Mejdi; Aouadi, Kaiss; Kadri, Adel. Category: ethers-buliding-blocks And the article was included in Journal of Molecular Structure in 2020. The article conveys some information:
Thirteen fused pyridine derivatives have been designed, synthesized. Their in vitro antimicrobial activity was investigated against some pathogenic bacteria and fungi and the majority of them showed excellent to moderate activity, especially compounds I and II displaying the potent inhibitory effect against K. pneumoniae with MIC values of 2.44 mM and 8.10 mM, resp. Their pharmacokinetic assessment also revealed promising druglikeness characteristics and ADME properties. The binding interactions of the most active analogs were performed through mol. docking against Staphylococcus aureus tyrosyl-tRNA synthetase. Results revealed that the enhanced activity of compound I can be modulated by the establishment, in 10-tyrosyltRNA synthetase complex, of hydrogen bond interactions between the lone pair of sulfur atom of the thiophen-3-amine ring and the hydrogen atom of the hydroxyl group of TYR 170 of 3.80 Å . These findings suggest that analogs I and II can be served as best candidates for designing and discovering of novel antimicrobial agents. In the experiment, the researchers used many compounds, for example, N,N-Dimethylformamide Dimethyl Acetal(cas: 4637-24-5Category: ethers-buliding-blocks)
N,N-Dimethylformamide Dimethyl Acetal(cas: 4637-24-5) belongs to anime. Reduction of nitro compounds, RNO2, by hydrogen or other reducing agents produces primary amines cleanly (i.e., without a mixture of products), but the method is mostly used for aromatic amines because of the limited availability of aliphatic nitro compounds. Reduction of nitriles and oximes (R2C=NOH) also yields primary amines.Category: ethers-buliding-blocks
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