118-92-3Relevant articles and documents
Synthesis of oxazolidinones from N-aryl-carbamate and epichlorohydrin under mild conditions
Buscemi, Silvestre,Insuasty, Braulio,Marzullo, Paola,Moreno, Leydi Marcela,Piccionello, Antonio Palumbo
supporting information, p. 140 - 155 (2022/03/27)
The reaction conditions for an enantiospecific synthesis of various N-aryl-oxazolidinones from N-aryl-carbamates and (R) or (S) epichlorohydrin were optimized. The N-aryl-oxazolidinones were applied to the synthesis of compounds of biological interest such as DuP 721, toloxatone and a linezolid analogue.
Discovery of Novel Tacrine-Pyrimidone Hybrids as Potent Dual AChE/GSK-3 Inhibitors for the Treatment of Alzheimer's Disease
Yao, Hong,Uras, Giuseppe,Zhang, Pengfei,Xu, Shengtao,Yin, Ying,Liu, Jie,Qin, Shuai,Li, Xinuo,Allen, Stephanie,Bai, Renren,Gong, Qi,Zhang, Haiyan,Zhu, Zheying,Xu, Jinyi
supporting information, p. 7483 - 7506 (2021/06/28)
Based on a multitarget strategy, a series of novel tacrine-pyrimidone hybrids were identified for the potential treatment of Alzheimer's disease (AD). Biological evaluation results demonstrated that these hybrids exhibited significant inhibitory activities toward acetylcholinesterase (AChE) and glycogen synthase kinase 3 (GSK-3). The optimal compound 27g possessed excellent dual AChE/GSK-3 inhibition both in terms of potency and equilibrium (AChE: IC50 = 51.1 nM; GSK-3β: IC50 = 89.3 nM) and displayed significant amelioration on cognitive deficits in scopolamine-induced amnesia mice and efficient reduction against phosphorylation of tau protein on Ser-199 and Ser-396 sites in glyceraldehyde (GA)-stimulated differentiated SH-SY5Y cells. Furthermore, compound 27g exhibited eligible pharmacokinetic properties, good kinase selectivity, and moderate neuroprotection against GA-induced reduction in cell viability and neurite damage in SH-SY5Y-derived neurons. The multifunctional profiles of compound 27g suggest that it deserves further investigation as a promising lead for the prospective treatment of AD.
Benzoselenazolone compound and application thereof and bactericide
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Paragraph 0090; 0119; 0120; 0122, (2021/01/24)
The invention relates to the field of antifungal drugs, and discloses a benzoselenazolone compound and application thereof and a bactericide, and the benzoselenazolone compound has a structural general formula shown in a formula (I). The benzoselenazolone compound provided by the invention can take candida albicans fructose-1, 6-diphosphate aldolase (Ca-FBA-II) as a target spot to inhibit the activity of the candida albicans fructose 1, 6-diphosphate aldolase (Ca-FBA-II), and has a good resistance effect on drug-resistant bacteria generated by taking cytochrome P450 as an action target.