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Facile Synthesis of Enantiomerically Pure 1-（5-Bromo-2-chlorophenyl）-1-（4-ethoxyphenyl）ethane

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Chemical Research in Chinese Universities 2014年第2期30卷 250-256页

作者： ZHANG Shuo WANG Wenjin LI Chuan LIU Peng xu weiren TANG Lida WANG Jianwu ZHAO Guilong School of Chemistry and Chemical Engineering Shandong University Jinan 250100 P.R.China Tianjin Key Laboratory of Molecular Design and Drug Discovery Tianjin Institute of Pharmaceutical ResearchTianjin 300193 P.R.China

A facile 7-step procedure for the synthesis of enantiomerically pure 1-（5-bromo-2-chlorophenyl）-1-（4-ethoxyphenyl）ethanes[（R）-2 and（S）-2] that started from （5-bromo-2-chlorophenyl）（4-ethoxyphenyl）methanone 3 was *** key step was the resolution of 2-（5-bromo-2-chlorophenyl）-2-（4-ethoxyphenyl）acetic acid 6 by crystallizations of its L-and D-menthyl esters 7 and 8 from petroleum ether to give optically pure enantiomers 9 and 10,*** absolute configurations of the products were unambiguously determined by single-crystal X-ray diffractions of four key intermediates,9,10,13 and *** procedure is characterized by inexpensiveness,scalability and ability to produce two individual enantiomers of a diarylethane with unambiguously determined absolute configurations and high enantiomeric purities.

关键词： Diarylethane Diastereomer Enantiomer Resolution SGLT2 inhibitor

3-Oxodapagliflozin as a Potent and Highly Selective SGLT2 Inhibitor for the Treatment of Type 2 Diabetes

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Chemical Research in Chinese Universities 2014年第5期30卷 785-793页

作者： ZHANG Shuo WANG Yuli LIU Wei XIE Yafei LIU Yuqiang xu weiren TANG Lida WANG Jianwua ZHAO Guilong School of Chemistry and Chemical Engineering Shandong University Jinan 250100 P. R. China Tianjin Key Laboratory of Molecular Design and Drug Discovery Tianjin Institute of Pharmaceutical Research Tianjin 300193 P. R. China

Structural modifications of 3-OH in the glucose moiety of dapagliflozin（1）, an approved potent sodium-dependent glucose transporter 2（SGLT2） inhibitor, led to 3-oxodapagliflozin（16）, a highly potent and more selective SGLT2 inhibitor[IC50（hSGLT1）/IC50（hSGLT2）=2851 for compound 16 vs. 843 for compound 1]. 3-Oxodapagliflozin（16） exhibited in vitro（IC50=1.0nmol/L against hSGLT2 for compound 16 vs. 1.3 nmol/L for compound 1） and in vivo activities comparable to those of dapagliflozin（1）. The bioactivities of 3-oxodapagliflozin （16） warrant its further evaluation as a promising SGLT2 inhibitor for the treatment of type 2 diabetes.

关键词： SGLT2 inhibitor Structure-activity relationship Dapagliflozin

Design, Synthesis and Biological Activity of Tetrazole-bearing Uric Acid Transporter 1 Inhibitors

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Chemical Research in Chinese Universities 2017年第1期33卷 49-60页

作者： CAI Wenqing LIU Wei XIE Yafei WU Jingwei LIU Yuqiang LIU Changying xu weiren TANG Lida WANG Jianwu ZHAO Guilong School of Chemistry and Chemical Engineering Shandong University Jinan 250100 P. R. China Tianjin Key Laboratory of Molecular Design and Drug Discovery Tianjin Institute of Pharmaceutical Research Tianjin 300193 P. R. China

Systematic structure-activity relationship（SAR） exploration of a moderately active tetrazole-bearmg lesinurad-based hit If led to the discovery of a potent uric acid transporter I（URAT1） inhibitor li, which possessed a novel molecular skeleton and was 11-fold more potent than the parent lesinurad against human URAT1 in-vitro （IC50=0.66 gmol/L for li vs. 7.18 μmol/L for lesinurad）.

关键词： URAT1 inhibitor Structure-activity relationship Drug discovery Lesinurad Tetrazole Bioisostere

The influence of genetic polymorphisms in drug metabolism enzymes and transporters on the pharmacokinetics of different fluvastatin formulations

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Asian Journal of Pharmaceutical Sciences 2020年第2期15卷 264-272页

作者： Qian Xiang Weidang Wu Nan Zhao Chuan Li Junyu xu Lingyue Ma Xiaodan Zhang Qiufen Xie Zhuo Zhang Jiancheng Wang weiren xu Xia Zhao Yimin Cui Department of Pharmacy Peking University First HospitalBeijing 100034China State Key Laboratory of Drug Release Technology and Pharmacokinetics Tianjin Institute of Pharmaceutical ResearchTianjin 300193China School of Pharmaceutical Science Peking UniversityBeijing 100191China

The purpose of the present study was to investigate the impact of genetic polymorphism on fluvastatin *** addition,we compared the fluvastatin pharmacokinetics differences between extended-release(ER)80 mg tablet and immediate-release(IR)40 mg capsule in terms of drug metabolism enzyme and transporter genetic *** this open-label,randomized,two-period,two-treatment,crossover study(n=24),effects of ABCG2,SLCO1B1,ABCB1,CYP2C9 and CYP3A5 polymorphisms on the pharmacokinetics of fluvastatin were *** administration dosage for IR 40 mg and ER 80 mg were twice and once daily,respectively,for total 7 *** samples for pharmacokinetic evaluation were taken on the 1st and 7th *** lower exposure following ER was *** ER tablets,SLCO1B1 T521C genotype correlated with AUC 0-24 of repeat doses(P=0.010).SLCO1B1 T521C genotype had no statistically significant effect on AUC 0-24 of IR capsule of fluvastatin after single or repeated *** vitro study demonstrated that when the concentration of fluvastatin was low(1μmol/l),transport velocity of fluvastatin by HEK293-OATP1B1 with SLCO1B1521TT(K m=11.4μmol/l)and with SLCO1B1521TCC(K m=15.1μmol/l)tend to be the *** suggests that the increased effect of SLCO1B1 T521C genotype on ER formulation of fluvastatin was mainly caused by lower blood *** recommend that formulation should be incorporated into future pharmacogenomics studies.

关键词： Genetic polymorphisms SLCO1B1 Fluvastatin Immediate-release Extended-release

The effects of local anesthetics on intracellular Ca^(2+) release from ryanodine-sensitive Ca^(2+) stores in gerbil hippocampal neurons

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Chinese Medical Journal 2002年第10期115卷 102-104,153-154页

作者：陈俊峰徐伟人蒋豪上海市长宁区中心医院麻醉科上海20036 复旦大学附属中山医院麻醉科上海200032

To examine the effects of procaine and lidocaine on intracellular Ca 2+ release from sarcoplasmic reticulum ryanodine sensitive Ca 2+ stores Methods The experiment was performed on hippocampal slices from 60-80 g male Mongolian gerbils Levels of intracellular Ca 2+ concentration in the slices were measured by microfluorometry The slices were perfused with 50 mmol/L KCl containing medium for 30 seconds Then, the medium was switched to physiological medium After 5 min of incubation, the slice was perfused with 20 mmol/L caffeine containing physiology medium for 2 min Following incubation, the slice was superfused with physiological medium until the end of the experiment The effects of procaine and lidocanin (100 μmol/L) on caffeine evoked Ca 2+ release were evaluated by adding them to the medium after high K + medium perfusion Results Caffeine induced a marked increase in intracellular Ca 2+ concentration which was then decreased 12% upon the addition of procaine ( P <0 05); however, lidocaine, did not induce a similar inhibitory reaction Conclusion Procaine inhibits ryanodine receptor mediated Ca 2+ release from intracellular Ca 2+ stores, while lidocaine may inhibit Ca 2+ release through other mechanisms

关键词： procaine · lidocaine · caffeine · gerbi l · hippocampus

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论网络教育的利弊与完善

中国远程教育 2001年第8期 16-19页

作者：周扬徐为人扬州广播电视大学计算机系 225002 国家税务总局扬州培训中心教学科研部

本文将网络教育界定为信息化带动的教育工业化实践，认为其优势与缺陷同出一源，都来自网络教育的工业化提供方式和“四大分离”固有特性，并在此基础上提出了扬长避短的五项完善措施。

关键词：教育工业化网络教育本质教育形式远程教育交互式教学

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钢轨闪光对接焊机焊接自动化的实现

上海铁道科技 2006年第1期 10-11,30页

作者：徐伟人上海铁路局科学技术研究所

近十年来，我国引进了多台K系列钢轨闪光对接焊机，上海铁路局科研所参加的K900钢轨焊机国产化工作也取得了成功。其中笔者负责了焊机的焊接控制程序和管理程序的设计。本文将介绍K系列钢轨闪光对接焊机的一些研究心得和国产钢轨焊机自... 详细信息

近十年来，我国引进了多台K系列钢轨闪光对接焊机，上海铁路局科研所参加的K900钢轨焊机国产化工作也取得了成功。其中笔者负责了焊机的焊接控制程序和管理程序的设计。本文将介绍K系列钢轨闪光对接焊机的一些研究心得和国产钢轨焊机自动化的主要控制原理，希望这有助于钢轨焊机的技术管理人员和使用人员用好焊机，更快地调整好焊接工艺参数，确保钢轨的焊接质量。

关键词：焊接自动化钢轨焊机对接闪光国产化工作焊接工艺参数上海铁路局管理程序控制程序控制原理

含噻二唑环的硫代糖苷类SGLT2抑制剂的设计、合成与降血糖活性研究

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有机化学 2010年第6期30卷 849-859页

作者：王致峰赵桂龙刘巍王玉丽邵华徐为人田来进曲阜师范大学化学与化工学院曲阜273165 天津药物研究院分子设计与药物发现天津市重点实验室天津300193

在相转移催化剂BnEt3N+Br-作用下,利用5-取代苯氧甲基-2-巯基-1,3,4-噻二唑与α-溴代四乙酰基吡喃糖室温反应,合成了22个结构新颖的硫代糖苷类SGLT2抑制剂化合物,结构经IR,1HNMR,13CNMR和HR-ESI-MS谱表征确认.采用小鼠口服葡萄糖耐受量... 详细信息

在相转移催化剂BnEt3N+Br-作用下,利用5-取代苯氧甲基-2-巯基-1,3,4-噻二唑与α-溴代四乙酰基吡喃糖室温反应,合成了22个结构新颖的硫代糖苷类SGLT2抑制剂化合物,结构经IR,1HNMR,13CNMR和HR-ESI-MS谱表征确认.采用小鼠口服葡萄糖耐受量法测定了目标化合物在治疗糖尿病方面的活性,结果发现化合物9Ah有明显的降糖作用,而9Aa和9Bi与对照药物格列齐特相当.

关键词：噻二唑硫代糖苷 SGLT2抑制剂合成降糖活性

体育院系学生篮球裁判员临场心理素质的调查与对策研究

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吉林体育学院学报 2007年第6期23卷 99-100页

作者：张明徐为人南京体育学院运动系江苏南京210014

通过对体育院系学生裁判员在临场执法的过程中产生心理压力的成因进行调查分析,并提出相应的对策。篮球裁判员的临场心理素质培养,要通过加强业务学习、要有充分的自信心、要有意识的进行心理调节、开好准备会和重视赛后小结、教师的有... 详细信息

通过对体育院系学生裁判员在临场执法的过程中产生心理压力的成因进行调查分析,并提出相应的对策。篮球裁判员的临场心理素质培养,要通过加强业务学习、要有充分的自信心、要有意识的进行心理调节、开好准备会和重视赛后小结、教师的有效疏导这几方面来进行。

关键词：学生篮球裁判员临场心理素质