Chemical & Pharmaceutical Bulletin
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#1Guo-liang Bai (Capital Medical University)
#2Tiantian Wu (NUAA: Nanjing University of Aeronautics and Astronautics)
Last. Xin Ni (Capital Medical University)H-Index: 1
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Bitter tastes are innately aversive and are thought to help protect animals from consuming poisons. Children are extremely sensitive to drug tastes, and their compliance is especially poor with bitter medicine. Therefore, judging whether a drug is bitter and adopting flavor correction and taste-masking strategies are key to solving the problem of drug compliance in children. Although various machine learning models for bitterness and sweetness prediction have been reported in the literature, no ...
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This account summarizes the development of a benzyne-mediated cyclization/functionalization protocol for the versatile construction of highly substituted benzene derivatives fused with an N-heterocyclic ring such as indolines, indoles, and related nitrogen-containing heterocycles. The protocol comprises sequential reactions initiated by generating a benzyne species and subsequent cyclization via addition of magnesium amide to the benzyne, followed by trapping of the resultant magnesium compound ...
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#1Miyu Furugoori (Showa Pharmaceutical University)
#2Kiwamu Yoshida (Showa Pharmaceutical University)
Last. Osamu Tamura (Showa Pharmaceutical University)H-Index: 28
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α,β-Unsaturated oximes underwent electrophilic epoxidation with in-situ-generated dimethyldioxirane to give the corresponding epoxides in good yields. This reaction is an example of "carbonyl umpolung" by transformation of α,β-unsaturated ketones to their oximes. Nucleophilic ring-opening reactions of the epoxides afforded α-substituted products. Shi asymmetric epoxidation of the oximes proceeded with moderate asymmetric selectivity.
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Last. Hongyan Liu (SDUTCM: Shandong University of Traditional Chinese Medicine)
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Yellow Croaker Ear-stone or Yunaoshi, is actually two kinds of fish otolith in China and has received increased attention in recent years as important folk medicine. For better understanding of this crude drug, a chaotic market circulation status investigation was carried out and seventeen samples with different varieties or producing areas were collected. In this study, pharmacodynamic components of nineteen varieties mineral elements of the seventeen samples were simultaneous determined by Ind...
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#1Yu Qian (SEU: Southeast University)
#2Lu Zhang (SEU: Southeast University)
Last. Yihong Wang (SEU: Southeast University)
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Preservatives in eye drops have always been the focus of people's attention. Benzalkonium chloride (BAC) is one of the most frequently used bacteriostatic agents in eye drops, which has broad-spectrum and efficient bactericidal ability. However, the inappropriate dosage of BAC may lead to high cytotoxicity. Therefore, adding low-toxic hydroxypropyltrimethyl ammonium chloride chitosan (HACC) can not only achieve antimicrobial effect, but also have the advantages of moisturizing and biocompatibili...
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Biomembranes are important targets in molecular design. Our laboratory has been exploring the design of functional peptides that modulate membrane barrier function, lipid packing, and structure. Evaluation of the results obtained and analyses of cellular mechanisms have yielded peptides with more refined designs and functions. This review highlights the progress made in our laboratory towards the development of unique peptides that modulate membrane properties.
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#1Kenji Sugibayashi (Josai University)H-Index: 44
#2Mika Futaki (Josai University)H-Index: 2
Last. Hiroaki Todo (Josai University)H-Index: 21
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The purpose of the present study was to evaluate whether iontophoresis (IP) accelerates the intradermal migration rate of medium molecular weight drugs. Sodium polystyrene sulfonate (PSA) and fluorescein isothiocyanate-dextran (FD) were used as model medium molecular weight acidic and non-electrolyte drugs, respectively. Low molecular weight acid and non-electrolyte drugs were also used for comparison. Drug-loaded excised split-layered skin (SL skin) was used in the experiment. SL skin was prepa...
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#1Huang Mingqi (SEU: Southeast University)
#2Jinghui Ren (SEU: Southeast University)H-Index: 1
Last. Jin Cai (SEU: Southeast University)H-Index: 13
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Poly(ADP-ribose)polymerase (PARP) is a significant therapeutic target for the treatment of numerous human diseases. Olaparib has been approved as a PARP inhibitor. In this paper, a series of new compounds were designed and synthesized with Olaparib as the lead compound. In order to evaluate the inhibitory activities against PARP1 of the synthesized compounds, in vitro PARP1 inhibition assay and intracellular PARylation assay were conducted. The results showed that the inhibitory activities of th...
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#1Nwet Nwet Win (University of Toyama)H-Index: 12
#2Takeshi Kodama (University of Toyama)H-Index: 10
Last. Hiroyuki Morita (University of Toyama)H-Index: 26
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A new brominated pyrrolactam stylissaol A (1) together with four known analogues, 2-bromoaldisine, aldisine, spongiacidin D, and Z-hymenialdisine, were isolated from the EtOAc extract of marine sponge Stylissa massa collected in Myanmar. The absolute configuration at C-10 of 1 was determined as R by the electronic circular dichroism (ECD) data. Among the isolated compounds, 2-bromoaldisine showed anti-Viral Protein R (Vpr) activity against TREx-HeLa-Vpr cells with an effective dose of 10 µM and ...
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#1Chisato Yoshikawa (Showa Pharmaceutical University)H-Index: 2
#2Hiroaki Ishida (Showa Pharmaceutical University)H-Index: 4
Last. Toshimasa Itoh (Showa Pharmaceutical University)H-Index: 17
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The coumarin skeleton has been a focus of attention for many years, and its fluorescence properties vary depending on the substituents. Fluorescent coumarin derivatives are useful tools for many strategies have been developed for their synthesis. Although 7-diethylaminocoumarin has excellent fluorescence properties, it is unstable. We have developed a facile strategy for the synthesis of 7-diethylaminocoumarin derivatives by increasing the electrophilicity of the ynone moiety to promote nucleoph...
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