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| 1 | SELECTIVE DIMERIZATION OF BUTANAL TO BUTYL BUTYRATE CATALYZED BY LANTHANOCENE/n-BuLi SYSTEMS显示文摘SELECTIVEDIMERIZATIONOFBUTANALTOBUTYLBUTYRATECATALYZEDBYLANTHANOCENE/n-BuLiSYSTEMS￥FanXU,LiLuZHANG,MingYAO,YuanChenDING,ZhiMi... | Xu, F Zhang, LL Yao, YM Ding, YC Bai, ZM Shen, Q | 1995 | Chinese Chemical Letters1995，6，7： | 2 |
| 2 | Design,synthesis,and anti-inflammatory evaluation of a series of novel amino acid-binding 1,5-diarylpyrazole derivatives显示文摘Aim: To design and synthesize a series of novel amino acid-binding 1,5-diarylpyrazole derivatives, which are intended to act as prodrugs with better aqueous solubility than celecoxib, and which will exert potent anti-inflammatory activi-ties after being converted to their parent compounds in vivo. Methods: To introduce an amino acid, celecoxib analogs containing amino or methylamino group were synthesized first through multi-step chemical reactions. All the synthesized compounds were screened in an intact cell-based assay in vitro and in carrageenan-induced mouse paw edema in vivo. Some active compounds were selected for further evaluation in a carrageenan-induced rat paw edema model. The preliminary pharmacokinetics experiments were conducted using high performance liquid chromatography/mass spectrometry (HPLC/MS). Results: Celecoxib, 6 of the 1,5-diarylpyrazole class of celecoxib analogs, and their amino acid derivatives (hydrochloride salts) were synthesized. In vitro screening, the hydrochloride salts showed decreased inhibitory effects on cyclooxygenase (COX)- 1 and COX-2 compared with their parent compounds, but some exhibited potent anti-inflammatory activity in vivo. Compound 4a was selected for further evaluation, and its anti-inflammatory effect was equivalent to that of celecoxib after oral administration in the carrageenan-induced rat paw edema model. At three doses (25 mg/kg, 50 mg/kg, and 100 mg/kg) the percentage inhibition on edema was 20.7%, 52.6%, and 62.6% (for compound 4a) and 27.8%, 38.4%, and 40.1% (for celecoxib), respectively. Preliminary pharmacokinetic evaluations support the hypothesis that compound 4a was actually converted to its parent compound, compound 4. Conclusion: The compound bound with amino acid acts like prodrug, which can exert anti-inflammatory effect similar to celecoxib after being converted to its parent compound. This finding will be of great benefit in carrying out structural modifications of prodrug-like selective COX-2 inhibitors. | Li MH Yin LL Cai MJ Zhang WY Huang Y Wang X Zhu XZ Shen JK | 2005 | Acta Pharmacologica Sinica2005，26，7： | 2 |
| 3 | Roles of the prostaglandin E2 receptors EP subtypes in Alzheimer's disease显示文摘 | Wei LL Shen YD Zhang YC | 2010 | Neurosci Bull2010，26，1： | 1 |
| 4 | Pharmacokinetics, pharmacodynamics, and safety of exenatide in patients with type 2 diabetes mellitus 显示文摘 | Koherman OG Kim DD Shen L Ruggles JA Nielsen LL Fineman MS | 2005 | Am J Health Syst Pharm2005，62，2： | 1 |
| 5 | Critical Role of Histone Methylation in Tumor SuppressorGene Silencing in Colorectal Cancer显示文摘 | Kondo Y Shen LL | 2003 | Mol Cell Biol2003，23，1： | 1 |
| 6 | Acetazolamide and respiratory chemosensitivity to CO2 in the neonatal rat transverse medullary slice显示文摘 | Necakov A Peever JH Shen LL | 2002 | Respiratory Physiology & Neurobiology2002，132，： | 1 |
| 7 | Decreased expression of auto- phagy-related proteins in malignant epithelial ovarian cancer显示文摘 | Shen Y Li DD Wang LL | 2008 | Autophagy2008，4，8： | 1 |
| 8 | Ischemic postconditioning mediatescardioprotection via PI3 K/GSK - 3 p/p - catenin signaling pathway inischemic rat myocardium显示文摘 | Wu QL Shen T Shao LL | 2012 | Shock2012，38，2： | 1 |
| 9 | The 2-Pyridone Antibacterial Agents:8-Position Modifications显示文摘 | Anthony K Fung L Shen LL | 2001 | Curr Pharm Des2001，15，8： | 1 |
| 10 | Two FT orthologs fromPopu- lus simonii Carrire induce early flowering in Arabidopsis and poplar trees 显示文摘 | Shen LL ChenY Su X H | 2012 | Plant Cell Tiss Organ Cult2012，108，： | 1 |
| 11 | Analysis for load limitation of square-shaped silicon diaphragms显示文摘 | ZHAO LL XU CH SHEN G G | | 0，，50： | 1 |
| 12 | Effects of electroacupuncture on pressor response to angiotensin-(1-7) by amino acid release in the rostral ventrolateral medulla显示文摘 | Wang J Shen LL Cao YX Zhu DN | 2003 | Acupunct Electrother Res2003，28，： | 1 |
| 13 | Acupuncture treatment for hypertension:a case study显示文摘 | Zhang LL Shen PF Wang S | 2014 | Acupuncture in Medicine2014，32，1： | 1 |
| 14 | Quinolone interactions with DNA and DNA gyrsse显示文摘 | Shen LL | 2001 | Methods Mol Bid2001，95，： | 1 |
| 15 | The 2-pyridone antibacterial agents: bacterial topoisomerase inhibitors显示文摘 | Li Q Mitscher LA Shen LL | 2000 | Med Res Rev2000，20，： | 1 |
| 16 | Storage behavior of Chionanthus retusus seed and asynchronous development of the radicle and shoot apex during germination in relation to germi- nation inhibitors, including Abscisic Acid and four phenolic glucosides 显示文摘 | Chien CT Kuo-Huang LL Shen YC | 2004 | Plant Cell Physiol2004，45，： | 1 |
| 17 | Interferon-inducible IFI16,a negative regulator of cell growth,down-regulates expression of human telomerase reverse transcriptase(h TERT)gene显示文摘 | Song LL Ponomareva L Shen H | 2010 | PLo S One2010，，1： | 1 |
| 18 | Assessment of ischemiamodified albumin levels for emergency room diagnosis of acute coronary syndrome显示文摘 | Shen XL Lin C J Han LL | | 0，，： | 1 |
| 19 | Poly ( N-iso- propylacrylamide)-chitosan as thermosensitive in situ gel-forming system for ocular drug delivery 显示文摘 | Cao Y Zhang C Shen W Cheng Z Yu LL Ping Q | 2007 | J Control Release2007，120，3： | 1 |
| 20 | Type Ⅱ DNA Topoisomerases as Antibacterial Targets显示文摘 | Shen LL Chu DTW | 1996 | Curr Pharm Des1996，2，2： | 1 |
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