RSC Advances
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2014
·Vol. 4
·期 49
·25933-25939
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IF 3.708
Qingfeng Liu,Yansen Zhang,Zhiguo Zhang,Tongxin Liu,Lei Shi,Guisheng Zhang
This paper describes a highly efficient and facile transformation of substituted oxazolidin-2-ones to methylene-bridged 3,3′-bis(oxazolidin-2-one) derivatives in a mixture solvent of CH2Cl2 (DCM) and N,N-dimethylformamide (DMF) in the presence of NaH at ambient temperature. Isotopic labeling experiments indicated that the C of the bridged methylene group was derived from CH2Cl2 instead of DMF and other unknown substances in the NaH reagent (60% dispersion in mineral oil).
研究领域:
有机化学
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药物化学
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DOI
高影响因子
Asian Journal of Organic Chemistry
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2018
·Vol. 7
·期 8
·1626-1634
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IF 2.496
Wen-Jing Pan,Zhong-Xia Wang
Graphical Cut my bonds into pieces : The C−H benzylation of oxazoles and benzoxazoles with benzyl trimethylammonium triflates was performed under mild conditions via Pd-catalyzed C−H/C−N cleavage. The method exhibits a wide scope of substrates and good compatibility of functional groups. The C−H benzylation of oxazoles and benzoxazoles with benzylic ammonium triflates was performed in reasonable to good yields via Pd-catalyzed C−H/C−N cleavage. The method exhibits a wide scope of azoles and benzylic ammonium triflates. A range of functional groups including F, CF 3 , COOEt, C(O)NMe 2 , OMe, OPh, pyridyl and thienyl groups can be tolerated.
研究领域:
有机化学
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药物化学
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DOI
高影响因子
Sustainable Chemistry and Pharmacy
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2024
·
IF 5.5
Jiangxin Li,Yuheng Xie,Xin Wang,Cong Li,Juan Zhang
In recent years, researchers have paid great attention to the preparation of oxazolidinone . In this paper, an ionic solid catalyst, IL-OAc, was synthesized for the synthesis of oxazolidinone by the reaction of propylene carbonate and aniline. Its structure and physical and chemical characteristics were characterized by SEM, FT-IR, EDS , TG-DTA, BET and 1 H MAS NMR. The influence of reaction conditions on catalytic performance was optimized. Under the optimum reaction conditions, the conversion of aniline was as high as 92.4% and the yield of oxazolidinone was 84.7%. After 6 cycles, the catalytic performance did not decrease obviously. The reaction conditions were further determined by response surface method, and the fitting results were in good agreement with the experimental results.
研究领域:
化学工程
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催化科学
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DOI
高影响因子
JOURNAL OF ORGANOMETALLIC CHEMISTRY
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2022
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IF 2.345
Li Dai,Di Xu,Peng-Fei Song,Jun Zhang
Featured by abundant derivation and powerful catalytic activities, chiral catalysts and ligands with oxazolinyl ferrocenes core play a vital role in the area of enantioselective transformations. Despite great researches on phosphine ligands with oxazolinyl ferrocene silyl ether core have been broadly explored, the example of N,O -ferrocene compounds with identical core is rare. We herein disclosed the practical approaches to the preparation of planar chiral oxazolinyl hydroxyl ferrocene silyl ethers. Several available methods were employed for the establishment of the configuration on planar chirality , which considered as key parameter for the subsequent relative products. Furthermore, an array of N,O,O- tridentate ferrocenes was obtained through desilylation treated with TBAF. The absolute stereochemical configuration of the synthesized ferrocene derivatives was determined by X-ray diffraction.
研究领域:
有机化学
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催化化学
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DOI
高影响因子
Journal of Pharmaceutical Investigation
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2024
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IF 5.3
Zhou Limei,Shang Yunxia,Wang Yaru,Wei Xiaohui
Purpose Ulcerative colitis (UC) is a chronic and non-specific inflammatory bowel disease that poses a serious threat to individuals' health and lives. Notoginsenoside R1 (R1) alleviates various symptoms caused by UC effectively. However, the application of R1 is somewhat restricted due to its low bioavailability and nontargeted delivery in vivo. Consequently, it is imperative to develop novel strategies to overcome the aforementioned limitations and enhance the efficacy of this drug. To enhance R1's efficacy and targeting ability, polyethylene glycol poly (lactic-co-glycolic acid) nanoparticles loaded with R1 (R1@PEG–PLGA NPs) modified by transferrin (Tf) were prepared in this study and named R1@Tf–PEG–PLGA NPs. Methods R1@PEG–PLGA NPs and R1@Tf–PEG–PLGA NPs were prepared through nanoprecipitation, and the characterization methods were as follows: First, the surface morphology of the NPs was studied through transmission electron microscopy. Second, particle size, polydispersity index (PDI), and zeta potential were measured with a Malvern particle size analyzer, and the Tf grafting rate on the surface of the NPs was determined by using a bicinchoninic acid protein quantification kit. Third, high-performance liquid chromatography was used in determining the drug load (DL), entrapment efficiency (EE), and in vitro release of the prepared preparation. In addition, the fluorescence intensities of fluorescent-labeled NPs absorbed and ingested in Caco-2 cells were observed through in vitro experiments using fluorescence microscopy; the effects of incubation time, incubation temperature, and endocytosis inhibitors on the uptake of nanoparticles were compared; and the uptake-transport mechanism was explored. Finally, in vivo experiments were performed using the oxazolone (OXZ)-induced UC model in Sprague–Dawley (SD) rats to assess the pharmacodynamic effects and tissue distribution of the prepared NPs. Results The experimentally prepared R1@Tf–PEG–PLGA NPs were round particles with particle size and PDI of 153.50 ± 2.01 and 0.11 ± 0.01, respectively. In addition, the DL of R1@Tf-PEG-PLGA NPs was 24.26% ± 0.18%, and the EE was 50.32% ± 0.86%. Furthermore, R1@Tf–PEG–PLGA NPs had a slower cumulative release rate in vitro than R1 and R1@PEG–PLGA NPs. Fluorescence results showed that under the same conditions, Caco-2 cells took up more Tf-PEG–PLGA NPs than they took up PEG–PLGA NPs. Studies on the cellular uptake mechanism of absorption and uptake determined that the PEG–PLGA NPs entered the cells mainly through fovea-mediated endocytosis, whereas the Tf–PEG–PLGA NPs entered the cells mainly through fovea-mediated and lattice protein-mediated endocytosis. In vivo intestinal tissue distribution results in OXZ-induced SD rats showed that R1@Tf–PEG–PLGA NPs were more enriched in the colon than R1 and R1@PEG–PLGA NPs, and pharmacodynamic evaluation showed that R1@Tf–PEG–PLGA NPs exhibited more pronounced effects in ameliorating colonic injury. Conclusion R1@Tf–PEG–PLGA NPs showed significant colonic targeting and anti-UC effect, showing promising applications.
研究领域:
药学
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纳米技术
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炎症性肠病
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药物递送系统
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DOI
高影响因子
Scientific Reports
·
2022
·Vol. 12
·期 1
·1-15
·
IF 4.996
Dong Hao,Feng Chenjie,Cai Xiyunyi,Hao Yuanyuan,Gu Xinyue,Cai Lei,Wu Shuting,Chen Jiamin,Liu Zhou,Xie Wen,Lu Xuanren,Qian Hongfa,Liu Yulin,Cao Yiming,Zhu Junlin,Xu Jiayi,Zhou Yanjie,Ma Shuangyu,Yang Sha,Shi Yufeng,Yu Haojiang,Shi Minjie,Wang Yurong,Gu Harvest F.,Fan Lei,Wu Liang
7-Met, a derivative of soybean isoflavone, is a natural flavonoid compound that has been reported to have multiple signaling pathways regulation effects. This study investigated the therapeutic effects of 7-Met on mice with atopic dermatitis induced by fluorescein isothiocyanate (FITC), or oxazolone (OXZ). 7-Met ameliorated FITC or OXZ-induced atopic dermatitis symptoms by decreasing ear thickness, spleen index, mast cell activation, neutrophil infiltration and serum IgE levels in female BALB/c mice. In FITC-induced atopic dermatitis mice, 7-Met reduced Th1 cytokines production and regulated Th1/Th2 balance by downregulating the secretion of thymic stromal lymphopoietin (TSLP) via inactivation of the NF-κB pathway. In OXZ-induced atopic dermatitis, 7-Met functioned through the reduction of Th17 cytokine production. Our study showed that 7-Methoxyisoflavone alleviated atopic dermatitis by regulating multiple signaling pathways and downregulating chemokine production.
研究领域:
免疫学
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药理学
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皮肤病学
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产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）