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Xi:Irritant;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.
Conjugation of tacrine with genipin derivative not only enhances effects on AChE but also leads to autophagy against Alzheimer's disease
Lin, Rongtian,Rao, Shuwen,Li, Yanbing,Zhang, Lei,Xu, Liyu,He, Yepu,Liu, Zhijun,Chen, Heru
, (2020/12/21)
Seven tacrine/CHR21 conjugates have been designed and synthesized. Compound 8-7 was confirmed as the most active AChE inhibitor with IC50 value of 5.8 ± 1.4 nM, which was 7.72-fold stronger than tacrine. It was also shown as a strong BuChE inhibitor (IC50 value of 3.7 ± 1.3 nM). 8-7 was clearly highlighted not only as an excellent ChEs inhibitor, but also as a good modulator on protein expression of AChE, p53, Bax, Bcl-2, LC3, p62, and ULK, indicating its functions against programmed cell apoptosis and decrease of autophagy. 8-7 significantly reversed the glutamate-induced dysfunctions including excessive calcium influx and release from internal organelles, overproduction of nitric oxide (NO) and Aβ high molecular weight oligomer. This compound can penetrate blood?brain barrier (BBB). The in vivo hepatotoxicity assay indicated that 8-7 was much less toxic than tacrine. Altogether, these data strongly support that 8-7 is a potential multitarget-directed ligand (MTDL) for treating Alzheimer's disease (AD).
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.
A highly selective diarylethene fluorescence sensor of aluminum ion and its application
Fan, Congbin,Liu, Gang,Pu, Shouzhi,Wang, Huaxin,Zhao, Heng
, (2020/10/18)
A novel diarylethene derivative 1O with the unit of N-(2-(hydrazinecarbonyl)phenyl)benzamide was designed and synthesized successfully. The sensor showed excellent photochromism and specific fluorescent detection toward aluminum ion with rarely interfering. The emission intensity could increase nearly by 100 folds with aluminum ion and the color changed from dark to Aqua green. The low limit of detection (LOD) of 1O was determined as 3.26 × 10-8 mol L-1. Additionally, the sensor could be used in logic circuit and aluminum ion detection in untreated water.
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.
The Discovery of Novel ACA Derivatives as Specific TRPM2 Inhibitors that Reduce Ischemic Injury Both in Vitro and in Vivo
Zhang, Han,Yu, Peilin,Lin, Hongwei,Jin, Zefang,Zhao, Siqi,Zhang, Yi,Xu, Qingxia,Jin, Hongwei,Liu, Zhenming,Yang, Wei,Zhang, Liangren
, p. 3976 - 3996 (2021/05/04)
The transient receptor potential melastatin 2 (TRPM2) channel is associated with ischemia/reperfusion injury, inflammation, cancer, and neurodegenerative diseases. However, the limit of specific inhibitors impedes the development of TRPM2-targeted therapeutic agents. To discover more potent and selective TRPM2 inhibitors, 59 N-(p-amylcinnamoyl) anthranilic acid (ACA) derivatives were synthesized and evaluated using calcium imaging and electrophysiology approaches. Systematic structure-activity relationship studies resulted in some potent compounds inhibiting the TRPM2 channel with sub-micromolar half-maximal inhibitory concentration values. Among them, the preferred compound A23 exhibited TRPM2 selectivity over TRPM8 and TRPV1 channels as well as phospholipase A2 and showed neuroprotective activity in vitro. Following pharmacokinetic studies, A23 was further evaluated in a transient middle cerebral artery occlusion model in vivo, which significantly reduced cerebral infarction. These data indicate that A23 might serve as a useful tool for TRPM2-related research as well as a lead compound for the development of therapeutic agents for ischemic injury.
Expedient discovery for novel antifungal leads: 1,3,4-Oxadiazole derivatives bearing a quinazolin-4(3H)-one fragment
Chai, Jianqi,Chen, Min,Jin, Fei,Kong, Xiangyi,Wang, Xiaobin,Xue, Wei,Yang, Chunlong
, (2021/08/03)
Developing novel fungicide candidates are intensively promoted by the rapid emergences of resistant fungi that outbreak on agricultural production. Aiming to discovery novel antifungal leads, a series of 1,3,4-oxadiazole derivatives bearing a quinazolin-4(3H)-one fragment were constructed for evaluating their inhibition effects against phytopathogenic fungi in vitro and in vivo. Systematically structural optimizations generated the bioactive molecule I32 that was identified as a promising inhibitor against Rhizoctonia solani with the in vivo preventative effect of 58.63% at 200 μg/mL. The observations that were captured by scanning electron microscopy and transmission electron microscopy demonstrated that the bioactive molecule I32 could induce the sprawling growth of hyphae, the local shrinkage and rupture on hyphal surfaces, the extreme swelling of vacuoles, the striking distortions on cell walls, and the reduction of mitochondria numbers. The above results provided an indispensable complement for the discovery of antifungal lead bearing a quinazolin-4(3H)-one and 1,3,4-oxadiazole fragment.
Aluminum ion detection fluorescent probe based on bifunctional organic small molecule as matrix and preparation method and application thereof
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Paragraph 0095-0099, (2021/11/14)
The invention discloses an aluminum ion detection fluorescent probe based on a bifunctional organic small molecule as a matrix and a preparation method and application of the fluorescence probe, and the structural formula is shown I. To the invention, 1, 8 - naphthalimide and isoquinoline hydrazide or 2 - benzamide benzoyl hydrazine are used as fluorescent groups, and the prepared Schiff base type probe NIQ or NBP is prepared into a solution Al through condensation reaction. 3 + High sensitivity and high selectivity are exhibited, and at the same time, the structure is stable. The low toxicity and cell infiltration capability is strong, and the trace metal aluminum ions in the living Hela cells are successfully detected. The preparation method of the fluorescent probe is simple, the raw materials are easily available, the obtained product is solid powder, is easy to store, and has a high application development prospect.
1, 2, 4 - Oxadiazole Nrf2 activator - tacrine split product as well as preparation method and application thereof
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Paragraph 0019; 0040; 0045; 0047, (2021/11/06)
The invention discloses 1,oxadiazole Nrf2 activator - tacrine split products as well as a preparation method and application thereof. The invention relates to an acetylcholinesterase inhibitory activity. Nrf2 Activation activity, selective screening and Morris water maze test was carried out to evaluate the compound of general formula I, II, III for the treatment of's disease (in particular, severe's disease), found to have good in vitro, in vivo activity and extremely high selectivity, and can be used as a precursor substance for further development through selective inhibition of acetylcholinesterase and activation Nrf2.
Hydroxamic acid rearrangement method for O-amino aromatic acid
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Paragraph 0018-0026, (2021/09/29)
The invention relates to the field of organic functional new material chemicals, and discloses a novel process technology for preparation of a hydroxamic acid precursor body weight discharge method of a plurality of o-amino aromatic acids in the first time. These substances are well known dyes and pigment and pharmaceutical pesticide-related fields and have a wide range of critical fine chemicals.