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Asian Journal of pharmaceutical Sciences 2013年第2期8卷 104-109页

作者： Toshimasa Tsukamoto Kohei Hironaka Takuya Fujisawa Daiki Yamaguchi Kohei Tahara Yuichi Tozuka Hirofumi Takeuchi laboratory of pharmaceutical Engineering Gifu Pharmaceutical University1-25-4 Daigaku-nishiGifu 501-1196Japan laboratory of formulation design and pharmaceutical Technology Osaka University of Pharmaceutical SciencesOsakaJapan

The purpose of this study was to design a submicron-sized liposomal non-steroidal antiinflammatory drug(NSAID)preparation that targets the retina via topical instillation of eye ***(BRF)-loaded liposomes were prepared using the calcium acetate gradient *** sizes and encapsulation efficiencies were optimized by screening several liposome formulations of lipid,drug concentration,and buffer *** entrapment efficiency was greater than 90%using this method,and was low using conventional hydration *** initial BRF loading using the pH gradient method caused aggregation of *** circumvent aggregation,the negatively charged lipid dicetylphosphate was incorporated into liposomes,which formed anion layer preventing *** of BRF from liposomes was sustained for several hours depending on lipid concentration,inner water phase,initial drug amounts,and surface *** modification with chitosan(CS),a mucoadhesive cationic polymer,was achieved using electrostatic interactions of negatively charged *** optimal concentration of CS for evasion of liposome aggregation was 0.15%.

关键词： NSAIDs pH Gradient method Surface modification Chitosan Eye drop

Synthesis and antibacterial activity of novel 10,11-epoxy acylide erythromycin derivatives

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Chinese Chemical Letters 2013年第3期24卷 183-185页

作者： Ying Nie Yin Sun Qi-Dong You Experimental Center of pharmaceutical Science China Pharmaceutical University Jiangsu Key laboratory of Drug design and Optimization China Pharmaceutical University

A series of novel acylide derivatives have been synthesized from clarithromyc｜n A via a tacile procedure. The C-3 modifications involved replacing the natural C-3 cladinosyl group in clarithromycin core with different aryl-piperzine sidechain via chemical synthesis, Meanwhile a distinctive intermediate with 10,11-epoxy moiety was obtained, The structure and stereochemistry of this novel structure were confirmed via NMR and X-ray crystallography. Potential anti-bacterial activities against both Grampositive and Gram-negative bacteria were reported. Because of existence of C10,11-epoxide, these derivatives can be used as intermediates for further structural modification.

关键词： Epoxide acylide erythromycin derivativesSynthesisSingle-crystal X-ray diffractionResistance antibacterial activity

Concise synthesis of dopexamine dihydrochloride via benzyl protecting protocol

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Chinese Chemical Letters 2015年第3期26卷 357-360页

作者： Yan Guo Hua Zhang Hao Yan Hai-Long Xin Hong-Yan Shen You-Jun Xu School of pharmaceutical Engineering and Key Laboratory of Structure-Based Drug Design & Discovery (Ministry of Education)Shenyang Pharmaceutical University

Benzyl protecting protocol was first employed in two routes for the concise synthesis of dopexamine *** protecting group could be cleanly removed under mild condition and no unacceptable ion was brought to the final *** total yield of route I was 43.8% from phenylacetic acid,while it was 54.1% of route II from 2-（3,4-bis（benzyloxy）phenyl）acetic *** titration purity of the final product was more than 99.5%,while any single or total impurities met the known standard of the drug by HPLC *** measured residual palladium met an acceptable limit（〈1 ppm） as an API for injection.

关键词： removed protecting titration palladium concise benzyl dissolved concentrated acetic brought

Synthesis,Crystal Structure and Anticoagulant Activity of 5-Chloro-N-[[(5S)-2-oxo-3-[4-(2-oxopyridin-1(2H)-yl)phenyl]oxazolidin-5-yl]methyl]thiophene-2-carboxamide

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Chinese Journal of Structural Chemistry 2014年第7期33卷 1091-1095页

作者：刘巍袁静张士俊徐为人黄长江汤立达 Tianjin Key laboratory of Molecular design and Drug Discovery Tianjin Institute of Pharmaceutical Research

The title compound （zifaxaban 2, C20HI6C1N3O4S, Mr = 429.87） was synthesized and its crystal structure was determined by single-crystal X-ray diffraction. Zifaxaban crystallizes in monoclinic, space group P21 with a = 5.7900（12）, b = 13.086（3）, c = 12.889（3） A, β= 100.86（3）°, V = 959.1（3））k3, Z = 2, Dc= 1.489 g/cm3, F（000） = 444,μ= 0.342 mm-l, the final R = 0.0320 and wR = 0.0640 for 2717 observed reflections （I 〉 20（I）. The absolute configuration of the stereogenic center in the title compound was confirmed to be S by single-crystal X-ray diffraction. Four existing intermolecular hydrogen bonds help to stabilize the lattice and the molecule in the lattice to adopt an L-shape conformation. Zifaxaban was slightly more active than rivaroxaban 1 in in vitro assay against human FXa and therefore is promising as a drug candidate.

关键词： synthesis crystal structure oxazolidinone factor Xa inhibitor zifaxaban

Protein tyrosine phosphatase 1B inhibitory activities of ursane-type triterpenes from Chinese raspberry, fruits of Rubus chingii

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Chinese Journal of Natural Medicines 2019年第1期17卷 15-21页

作者： ZHANG Xiang-Yu LI Wei WANG Jian LI Ning CHENG Mao-Sheng KOIKE Kazuo Key laboratory of Structure-Based Drug design&Discovery Ministry of EducationShenyang Pharmaceutical University School of pharmaceutical Engineering Shenyang Pharmaceutical University Faculty of pharmaceutical Sciences Toho University

Protein tyrosine phosphatase 1 B(PTP1 B) has led to an intense interest in developing its inhibitors as anti-diabetes, anti-obesity and anti-cancer agents. The fruits of Rubus chingii(Chinese raspberry) were used as a kind of dietary traditional Chinese medicine. The methanolic extract of R. chingii fruits exhibited significant PTP1 B inhibitory activity. Further bioactivity-guided fractionation resulted in the isolation of three PTP1 B inhibitory ursane-type triterpenes: ursolic acid(1), 2-oxopomolic acid(2), and 2α, 19α-dihydroxy-3-oxo-urs-12-en-28-oic acid(3). Kinetics analyses revealed that 1 was a non-competitive PTP1 B inhibitor, and 2 and 3 were mixed type PTP1 B inhibitors. Compounds 1-3 and structurally related triterpenes(4-8) were further analyzed the structure-activity relationship, and were evaluated the inhibitory selectivity against four homologous protein tyrosine phosphatases(TCPTP, VHR, SHP-1 and SHP-2). Molecular docking simulations were also carried out, and the result indicated that 1, 3-acetoxyurs-12-ene-28-oic acid(5), and pomolic acid-3β-acetate(6) bound at the allosteric site including α3, α6, and α7 helix of PTP1 B.

关键词： Protein tyrosine phosphatase 1B Raspberry Rubus chingii Triterpene Ursane

Thin films as an emerging platform for drug delivery

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Asian Journal of pharmaceutical Sciences 2016年第5期11卷 559-574页

作者： Sandeep Karki Hyeongmin Kim Seon-Jeong Na Dohyun Shin Kanghee Joa Jaehwi Lee pharmaceutical formulation design laboratory College of PharmacyChung-Ang UniversitySeoul 06974Republic of Korea Bio-Integration Research Center for Nutra-pharmaceutical Epigenetics Chung-Ang UniversitySeoul 06974Republic of Korea Center for Metareceptome Research Chung-Ang UniversitySeoul 06974Republic of Korea

pharmaceutical scientists throughout the world are trying to explore thin films as a novel drug delivery tool. Thin films have been identified as an alternative approach to conventional dosage forms. The thin films are considered to be convenient to swallow, selfadministrable, and fast dissolving dosage form, all of which make it as a versatile platform for drug delivery. This delivery system has been used for both systemic and local action via several routes such as oral, buccal, sublingual, ocular, and transdermal routes. The design of efficient thin films requires a comprehensive knowledge of the pharmacological and pharmaceutical properties of drugs and polymers along with an appropriate selection of manufacturing processes. Therefore, the aim of this review is to provide an overview of the critical factors affecting the formulation of thin films, including the physico-chemical properties of polymers and drugs, anatomical and physiological constraints, as well as the characterization methods and quality specifications to circumvent the difficulties associated with formulation design. It also highlights the recent trends and perspectives to develop thin film products by various companies.

关键词： Thin film Film-forming polymer Mechanical properties Manufacturing Characterization

Non-invasive gene delivery across the blood-brain barrier:present and future perspectives

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Neural Regeneration Research 2022年第4期17卷 785-787页

作者： Seigo Kimura Hideyoshi Harashima laboratory for Molecular design of Pharmaceutics Faculty of Pharmaceutical SciencesHokkaido UniversitySapporoJapan laboratory of Innovative Nanomedicine Faculty of Pharmaceutical SciencesHokkaido UniversitySapporoJapan

The aging of society has arrived,and is accompanied by an increase in the absolute numbers of patients with neurological disorders,such as Alzheimer's and Parkinson's diseases(Feigin et al.,2020).Such diseases,particularly Alzheimer's disease and other forms of dementia,affect not only the patients themselves,but also the people around them,including family members and care *** a result,such neurological disorders are thought to carry a larger social burden compared to other *** most critical point in the current situation is that there is no effective treatment despite the fact that the number of patients increase with the aging of the population.

关键词： diseases Alzheimer carry

Synthesis and Crystal Structure of 2,3,4,6-tetra-O-Acetyl-1-{4-chloro-3-[1-(4-ethoxyphenyl)-1-methylethyl]phenyl}-1-deoxy-β-D-glucopyranose

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Chinese Journal of Structural Chemistry 2012年第5期31卷 690-694页

作者：史永恒赵桂龙邵华王玉丽刘巍汤立达 Tianjin Key laboratory of Molecular design and Drug Discovery Tianjin Institute of Pharmaceutical Research School of pharmaceutical Science Tianjin Medical University

The title compound was synthesized and its crystal structure was determined by single-crystal X-ray *** crystal is of monoclinic system（C31H37ClO10,Mr = 605.06）,space group P21 with a = 11.882（5）,b = 10.106（5）,c = 13.816（6）,V = 1545.9（12）（A°）^3,Z = 2,Dc = 1.300 g/cm^3,F（000） = 640,μ = 0.179 mm^-1,the final R = 0.0430 and wR = 0.0595 for 4960 observed reflections（I 〉 2σ（I））.The title compound was confirmed to be a β-anomer by single-crystal X-ray diffraction and 1H *** proximal benzene ring is nearly orthogonal to the glucopyranoside ring,and the two benzene rings are also almost orthogonal to each *** non-classical intermolecular hydrogen bonds observed in the crystal lattice help to stabilize the crystal.

关键词： synthesis crystal structure C-glucoside SGLT2 inhibitor gem-dimethyl

Synthesis and antitumor activities of a new series of 4,5-dihydro-1H-thiochromeno[4,3-d]pyrimidine derivatives

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Science China Chemistry 2012年第3期55卷 347-351页

作者： GUO DeXiang LIU YaJing LI Ting WANG Nan ZHAI Xin HU Chun GONG Ping Key laboratory of New Drugs design and Discovery of Liaoning Province School of Pharmaceutical EngineeringShenyang Pharmaceutical UniversityShenyang 110016China

A new series of 4,5-dihydro-lH-thiochromeno[4,3-d]pyrimidine derivatives have been designed and synthesized. The anti- tumor activities of the target compounds have been evaluated in vitro against two human cancer cell lines including A549 （human alveolar adenocarcinoma cell） and H460 （human lung cancer） by MTT assay. Most of the target compounds exhibited significant antitumor activities against A549 and H460 cancer cell lines. The most potent compound 4-（benzo[d][1,3]dioxol- 5-yl）-8,9-difluoro-2-（4-methylpiperazin-l-yl）-4,5-dihydro-1H-thiochromeno[4,3-d]pyrimidine （CH05）（IC50 = 0.44 μM, 3.07 μM） was 2.0 and 8.4 times more active than gefitinib （IC50= 0.89 μM, 16.81 μM） against A549 and H460 cell lines, respectively.

关键词： heterocycle synthesis 4 5-dihydro-lH-thiochromeno[4 3-d]pyrimidine derivatives antitumor activity

Crystal Structure of 3-(4-Methoxyphenyl)-2-(4-methylbenzoyl)-6,7-dihydro-5H-furo[3,2-g]chromene

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Chinese Journal of Structural Chemistry 2016年第4期35卷 545-549页

作者：李晗悦韩宇金辄王世辉李新增刘思宇胡春 Key laboratory of Structure-based Drug design & Discovery Ministry of Education Shenyang pharmaceutical University

The crystal structure of 3-（4-methoxyphenyl）-2-（4-methylbenzoyl）-6,7-dihydro-5H-furo[3,2-g]chromene was obtained by X-ray single-crystal diffraction. The molecule is in the triclinic crystal system, space group P1 with a = 11.0745（4）, b = 13.0953（7）, c = 15.8773（8）？, α = 92.811（4）, β = 104.815（4）, γ = 111.797（4）o, Z = 4, the final R = 0.0567 and w R = 0.1540. X-ray crystal structure data revealed that one asymmetric structure unit of the title compound contained two molecules. The existence of methyl group changed the dihedral angle between furan ring and the phenyl ring at the C2 position of the furo[3,2-g]chromene scaffold as well as the conformation, and had a further influence on the bioactivity of the furo[3,2-g]chromene derivatives.

关键词： furo[3 2-g]chromene crystal structure dihedral angle bioactivity