52727-95-4Relevant academic research and scientific papers
The synthesis and antistaphylococcal activity of 9, 13-disubstituted berberine derivatives
Wang, Jing,Yang, Teng,Chen, Huang,Xu, Yun-Nan,Yu, Li-Fang,Liu, Ting,Tang, Jie,Yi, Zhengfang,Yang, Cai-Guang,Xue, Wei,Yang, Fan
, p. 424 - 433 (2017)
A series of novel 9, 13-disubstituted berberine derivatives have been synthesized and evaluated for the antibacterial activities against Staphylococcus aureus, including Newman strain and multidrug-resistant strains (NRS-1, NRS-70, NRS-100, NRS-108, and NRS-271). Compound 20 shows the most potent activity against the growth of Newman strain, with a MIC value of 0.78?μg/mL, which is comparable with the positive control vancomycin. In addition, compound 20, 21, and 33 are highly antistaphylococcal active against five strains of multidrug-resistant S.?aureus, with MIC values of 0.78–1.56?μg/mL. Of note, theses antibacterial active compounds have no obvious toxicity to the viability of human fibroblast (HAF) cells at the MIC concentration.
Single AIEgen for Multiple Tasks: Imaging of Dual Organelles and Evaluation of Cell Viability
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Paragraph 0063; 0070-0071, (2021/04/17)
A fluorescent probe can include a compound exhibiting aggregation-induced emission (AIE). The probe can be used for selectively staining mitochondria and lipid droplets and detecting esterase activity. The probe includes an acetoxyl group which can be rec
Design, synthesis, and biological evaluation of dual targeting inhibitors of histone deacetylase 6/8 and bromodomain BRPF1
Erdmann, Frank,Günther, Stefan,Ghazy, Ehab,Hügle, Martin,Herp, Daniel,Jung, Manfred,Morales, Elizabeth R.,Robaa, Dina,Romier, Christophe,Schmidt, Matthias,Schmidtkunz, Karin,Sippl, Wolfgang,Zeyen, Patrik
, (2020/06/03)
Histone modifying proteins, specifically histone deacetylases (HDACs) and bromodomains, have emerged as novel promising targets for anticancer therapy. In the current work, based on available crystal structures and docking studies, we designed dual inhibitors of both HDAC6/8 and the bromodomain and PHD finger containing protein 1 (BRPF1). Biochemical and biophysical tests showed that compounds 23a,b and 37 are nanomolar inhibitors of both target proteins. Detailed structure-activity relationships were deduced for the synthesized inhibitors which were supported by extensive docking and molecular dynamics studies. Cellular testing in acute myeloid leukemia (AML) cells showed only a weak effect, most probably because of the poor permeability of the inhibitors. We also aimed to analyse the target engagement and the cellular activity of the novel inhibitors by determining the protein acetylation levels in cells by western blotting (tubulin vs histone acetylation), and by assessing their effects on various cancer cell lines.
A fluorogenic probe using a catalytic reaction for the detection of trace intracellular zinc
Takashima, Ippei,Inoue, Yohei,Matsumoto, Nobuyuki,Takagi, Akira,Okuda, Kensuke
supporting information, p. 13327 - 13330 (2020/11/10)
Labile zinc plays various roles in cells at low concentrations which most fluorescent probes are not able to detect. Here we report a cephem-based probe which coordinates to zinc and zinc-bound water cleaves the scaffold and releases the fluorophore. In addition, the zinc is recycled and reacts with multiple probes, amplifying the signal. This signal amplification system is useful for the detection of intracellular zinc at low concentrations and has potential for further development of probes with a similar molecular design. This journal is
3, 5-disubstituted hydantoin compound as well as preparation method and application thereof
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Paragraph 0042; 0073; 0074; 0077; 0078, (2018/10/19)
The invention provides a 3, 5-disubstituted hydantoin compound as well as a preparation method and an application thereof. The structure of the compound is shown in formula I in the description. The application of the 3, 5-disubstituted hydantoin compound shown in the formula I or solvates, hydrates or salts of the compound in preparation of medicines for treating Alzheimer's disease, vascular dementia and other dementia diseases with memory impairment also belongs to the protection scope. Animal experiments prove that the compound has the effect of saving memory of animal models, has high safety, does not have mutagenicity, can stay in blood for several hours after oral administration and intravenous injection, and can enter the brain.
Synthetic process of esmolol intermediate 3-(4-hydroxyphenyl) methyl propionate
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Paragraph 0020; 0023; 0025, (2018/11/03)
The invention belongs to the field of medicinal chemical industry, and particularly relates to a synthetic process of an esmolol intermediate 3-(4-hydroxyphenyl) methyl propionate. The synthetic process comprises the steps of: adopting p-methyl phenol and acetic anhydride as raw materials, performing an acylation reaction to obtain (4-methyl) phenol acetate, performing a halogenation reaction between the obtained (4-methyl) phenol acetate and a halogenating reagent, then carrying out a substitution reaction between the halogenated product and diethyl malonate, performing hydrolysis decarboxylation, and then carrying out an esterification reaction between the obtained product with methanol to obtain the 3-(4-hydroxyphenyl) methyl propionate. Through the route of the synthetic process, the process conditions are optimized, and the synthetic process has simple operation, easy and available raw materials and low cost; and the 3-(4-hydroxyphenyl) methyl propionate is obtained finally through acylation, halogenation, substitution, hydrolysis decarboxylation and the esterification reaction, and the synthetic process has a good industrial value and a total yield of 48.8%.
PRODRUGS OF HYDROXAMATE-BASED GCPII INHIBITORS
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Page/Page column 49; 63; 64, (2018/06/06)
Prodrugs of hydroxamate-based GCPII inhibitors and methods of their use for treating a disease or condition are disclosed.
4-oxo-alkylated tetramic acid compounds and preparation method thereof
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Paragraph 0102; 0103, (2017/12/09)
The invention relates to novel compounds and a preparation method thereof. The general structural formula is shown as formula I in the description. Animal experiments prove that the compounds have the effect of saving memories of animal models, are high in safety, have no mutagenicity, can remain in blood for hours after oral administration and intravenous injection, can enter brains and can be used for preparing drugs for treating diseases such as Alzihemer's disease, Parkinson's disease, Huntington's disease, vascular dementia, schizophrenia, autism and the like.
4-oxo-alkylated tetramic acid compound as well as preparation method and application thereof
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Paragraph 0103; 0104, (2018/01/09)
The invention relates to a novel compound as well as preparation method and application thereof. The structural formula of the novel compound is as shown in a formula I. Animal tests show that the compound provided by the invention has a memory effect of rescuing animal models, is high in security and free of mutagenicity induction, can be retained for hours in blood after oral taking and intravenous injection, can be fed into brains and can be used for preparing medicines for treating senile dementia, Parkinsonism, Huntington diseases, vascular dementia, schizophrenia, autism and the like.
Palladium-catalyzed silylation reaction between benzylic halides and silylboronate
Huang, Zhi-Dao,Ding, Ran,Wang, Peng,Xu, Yun-He,Loh, Teck-Peng
supporting information, p. 5609 - 5612 (2016/05/09)
An efficient Pd-catalyzed silylation reaction of benzylic halides with silylboronate is reported. In this reaction, primary and secondary benzylic halides could react well with silylboronates to afford benzylic silanes. This reaction accommodates a broad substrate scope and proceeds smoothly under very mild reaction conditions. The corresponding products could be obtained in moderate to high yields and with stereospecificity.
