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文章名     作者     期刊名     摘要     卷     期         如果没有找到您所需要的文献，请点击 ——此处申请     共36条记录   Novel Spirotetracyclic Zwitterionic Dual H-1/5-HT2A Receptor Antagonists for the Treatment of Sleep Disorders [作者：GIANOTTI MASSIMO; BOTTA MAURIZIO; BROUGH STEPHEN; CARLETTI RENZO; CASTIGLIONI EMILIANO; CORTI CORRADO; DALCIN MICHELE; DELLE FRATTE SONIA; KORAJAC DENANA; LOVRIC MARIJA; MERLO GIANCARLO; MESIC MILAN; PAVONE FRANCESCA; PICCOLI LAURA; RAST SLAVKO; ROSCIC MAJA; SAVA ANNA; SMEHIL MARIO; STASI LUIGI; TOGNINELLI ANDREA; WIGGLESWORTH MARK J,期刊：Journal of Medicinal Chemistry, 页码：7778-7795 , 文章类型： Article，,卷期：2010年53-21] Histamine H-1 and serotonin 5-HT2A receptors mediate two different mechanisms involved in sleep regulation: H-1 antagonists are sleep inducers, while 5-HT2A antagonists are sleep maintainers. Starting from 9'a, a novel s... Cationic Porphycenes as Potential Photosensitizers for Antimicrobial Photodynamic Therapy [作者：RAGAS XAVIER; SANCHEZGARCIA DAVID; RUIZGONZALEZ RUBEN; DAI TIANHONG; AGUT MONTSERRAT; HAMBLIN MICHAEL R; NONELL SANTI,期刊：Journal of Medicinal Chemistry, 页码：7796-7803 , 文章类型： Article，,卷期：2010年53-21] Structures of typical photosensitizers used in antimicrobial photodynamic therapy are based on porphyrins, phthalocyanines, and phenothiazinium salts, with cationic charges at physiological pH values. However, derivative... Exploration of the Active Site of Neuronal Nitric Oxide Synthase by the Design and Synthesis of Pyrrolidinomethyl 2-Aminopyridine Derivatives [作者：JI HAITAO; DELKER SILVIA L; LI HUIYING; MARTASEK PAVEL; ROMAN LINDA J; POULOS THOMAS L; SILVERMAN RICHARD B,期刊：Journal of Medicinal Chemistry, 页码：7804-7824 , 文章类型： Article，,卷期：2010年53-21] Neuronal nitric oxide synthase (nNOS) represents an important therapeutic target for the prevention of brain injury and the treatment of various neurodegenerative disorders. A series of trans-substituted amino pyrrolidin... Fruitful Adrenergic alpha(2C)-Agonism/alpha(2A)-Antagonism Combination to Prevent and Contrast Morphine Tolerance and Dependence [作者：DEL BELLO FABIO; MATTIOLI LAURA; GHELFI FRANCESCA; GIANNELLA MARIO; PIERGENTILI ALESSANDRO; QUAGLIA WILMA; CARDINALETTI CLAUDIA; PERFUMI MARINA; THOMAS RUSSELL J; ZANELLI UGO; MARCHIORO CARLA; DAL CIN MICHELE; PIGINI MARIA,期刊：Journal of Medicinal Chemistry, 页码：7825-7835 , 文章类型： Article，,卷期：2010年53-21] The functional in vitro study of the enantiomers of imidazolines 4-7 highlighted the role played by the nature of the ortho phenyl substituent in determining the preferred alpha(2C)-AR configuration. Indeed, the (S) enan... Rational Design, Synthesis, and Evaluation of New Selective Inhibitors of Microbial Class II (Zinc Dependent) Fructose Bis-phosphate Aldolases [作者：DAHER RACHA; COINCON MATHIEU; FONVIELLE MATTHIEU; GEST PETRA M; GUERIN MARCELO E; JACKSON MARY; SYGUSCH JURGEN; THERISOD MICHEL,期刊：Journal of Medicinal Chemistry, 页码：7836-7842 , 文章类型： Article，,卷期：2010年53-21] We report the synthesis and biochemical evaluation of several selective inhibitors of class II (zinc dependent) fructose bis-phosphate aldolases (Fba). The products were designed as transition-state analogues of the cata... Synthetic Analogues of the Microtubule-Stabilizing Sponge Alkaloid Ceratamine A Are More Active than the Natural Product [作者：NODWELL MATT; ZIMMERMAN CARLA; ROBERGE MICHEL; ANDERSEN RAYMOND J,期刊：Journal of Medicinal Chemistry, 页码：7843-7851 , 文章类型： Article，,卷期：2010年53-21] Desbromoceratamine A (3) exhibits significantly less potent activity than the natural product ceratamine A (1) in a cell-based assay for antimitotic activity. Synthesis of the ceratamine A analogue 4 has shown that repla... Design, Synthesis, Crystal Structures, and Antimicrobial Activity of Sulfonamide Boronic Acids as beta-Lactamase Inhibitors [作者：EIDAM OLIV; ROMAGNOLI CHIARA; CASELLI EMILIA; BABAOGLU KERIM; POHLHAUS DENISE TEOTICO; KARPIAK JOEL; BONNET RICHARD; SHOICHET BRIAN K; PRATI FABIO,期刊：Journal of Medicinal Chemistry, 页码：7852-7863 , 文章类型： Article，,卷期：2010年53-21] We investigated a series of sulfonamide boronic acids that resulted from the merging of two unrelated AmpC beta-lactamase inhibitor series. The new boronic acids differed in the replacement of the canonical carboxamide, ... Design, Synthesis, and Development of Novel Guaianolide-Endoperoxides as Potential Antimalarial Agents [作者：SUN LINGZHI; SHAH FALGUN; HELAL MOHAMED A; WU YUNSHAN; PEDDURI YAKAMBRAM; CHITTIBOYINA AMAR G; GUT JIRI; ROSENTHAL PHILIP J; AVERY MITCHELL A,期刊：Journal of Medicinal Chemistry, 页码：7864-7868 , 文章类型： Article，,卷期：2010年53-21] Design and synthesis of a guaianolide-endoperoxide (thaperoxide) 3 was pursued as a new antimalarial lead which was found to be noncytotoxic as compared to the natural product lead thapsigargin 2. Several analogues of 3 ... Diaryldiamines with Dual Inhibition of the Histamine H-3 Receptor and the Norepinephrine Transporter and the Efficacy of 4-(3-(Methylamino)-1-phenylpropyl)-6-(2-(pyrrolidin-1-yl)ethoxy)naphthalen-1-ol in Pain [作者：ALTENBACH ROBERT J; BLACK LAWRENCE A; STRAKHOVA MARINA I; MANELLI ARLENE M; CARR TRACY L; MARSH KENNAN C; WETTER JILL M; WENSINK ERICA J; HSIEH GIN C; HONORE PRISCA; GARRISON TIFFANY RUNYAN; BRIONI JORGE D; COWART MARLON D,期刊：Journal of Medicinal Chemistry, 页码：7869-7873 , 文章类型： Article，,卷期：2010年53-21] A series of compounds was designed as dual inhibitors of the H-3 receptor and the norepinephrine transporter. Compound 5 (rNET K-i = 14 nM; rH(3)R K-i = 37 nM) was found to be efficacious in a rat model of osteoarthritic... Indazolylpyrazolopyrimidine as Highly Potent B-Raf Inhibitors with in Vivo Activity [作者：WANG XIAOLUN; BERGER DAN M; SALASKI EDWARD J; TORRES NANCY; DUTIA MINU; HANNA CILIEN; HU YONGBO; LEVIN JEREMY I; POWELL DENNIS; WOJCIECHOWICZ DONALD; COLLINS KAREN; FROMMER EILEEN; LUCAS JUDY,期刊：Journal of Medicinal Chemistry, 页码：7874-7878 , 文章类型： Article，,卷期：2010年53-21] Novel indazolylpyrazolo[1,5-a]pyrimidine analogues have been prepared and found to be extremely potent type I B-Raf inhibitors. The lead compound shows good selectivity against a panel of 60 kinases, possesses a desirabl... Properties and Synthesis of 2-{2-Fluoro (or Bromo)-4-[(2-oxocyclopentyl)methyl]phenyl}propanoic Acid: Nonsteroidal Anti-inflammatory Drugs with Low Membrane Permeabilizing and Gastric Lesion-Producing Activities [作者：YAMAKAWA NAOKI; SUEMASU SHINTARO; MATOYAMA MASAAKI; KIMOTO AYUMI; TAKEDA MIHO; TANAKA KENICHIRO; ISHIHARA TOMOAKI; KATSU TAKASHI; OKAMOTO YOSHINARI; OTSUKA MASAMI; MIZUSHIMA TOHRU,期刊：Journal of Medicinal Chemistry, 页码：7879-7882 , 文章类型： Article，,卷期：2010年53-21] We previously proposed that membrane permeabilization activity of NSAIDs is involved in NSAID-induced gastric lesions. We here synthesized derivatives of loxoprofen that have lower membrane permeabilization activity than... Corrections to Falcipain Inhibitors: Optimization Studies of the 2-Pyrimidinecarbonitrile Lead Series (vol 53, pg 6129, 2010) [作者：COTERON JOSE M; CATTERICK DAVID; CASTRO JULIA; CHAPARRO MARIA J; DIAZ BEATRIZ; FERNANDEZ ESTHER; FERRER SANTIAGO; GAMO FRANCISCO J; GORDO MARIOLA; GUT JIRI; DE LAS HERAS LAURA; LEGAC JENNIFER; MARCO MARIA; MIGUEL JUAN; MUNOZ VICENTE; PORRAS ESTHER; DE LA ROSA JUAN C; RUIZ JOSE R; SANDOVAL ELENA; VENTOSA PILAR; ROSENTHAL PHILIP J; FIANDOR JOSE M,期刊：Journal of Medicinal Chemistry, 页码：7885-7886 , 文章类型： Correction，,卷期：2010年53-21] Medicinal Chemistry as a Conduit for the Modulation of Quorum Sensing [作者：LOWERY COLIN A; SALZAMEDA NICHOLAS T; SAWADA DAISUKE; KAUFMANN GUNNAR F; JANDA KIM D,期刊：Journal of Medicinal Chemistry, 页码：7467-7489 , 文章类型： Article，,卷期：2010年53-21] Direct Renin Inhibitors as a New Therapy for Hypertension [作者：WEBB RANDY L; SCHIERING NIKOLAUS; SEDRANI RICHARD; MAIBAUM JUERGEN,期刊：Journal of Medicinal Chemistry, 页码：7490-7520 , 文章类型： Article，,卷期：2010年53-21] Selection of Evodiamine as a Novel Topoisomerase I Inhibitor by Structure-Based Virtual Screening and Hit Optimization of Evodiamine Derivatives as Antitumor Agents [作者：DONG GUOQIANG; SHENG CHUNQUAN; WANG SHENGZHENG; MIAO ZHENYUAN; YAO JIANZHONG; ZHANG WANNIAN,期刊：Journal of Medicinal Chemistry, 页码：7521-7531 , 文章类型： Article，,卷期：2010年53-21] Human topoisomerase I (TopoI) is recognized as a valuable target for the development of effective antitumor agents. Structure-based virtual screening was applied to the discovery of structurally diverse TopoI inhibitors.... New Fluoro Derivatives of the Pyrazolo[5,1-c][1,2,4]benzotriazine 5-Oxide System: Evaluation of Fluorine Binding Properties in the Benzodiazepine Site on gamma-Aminobutyrric Acid Type A (GABA(A)) Receptor. Design, Synthesis, Biological, and Molecular Modeling Investigation [作者：GUERRINI GABRIELLA; CICIANI GIOVANNA; BRUNI FABRIZIO; SELLERI SILVIA; GUARINO CHIARA; MELANI FABRIZIO; MONTALI MARINA; DANIELE SIMONA; MARTINI CLAUDIA; GHELARDINI CARLA; NORCINI MONICA; CIATTINI SAMUELE; COSTANZO ANNARELLA,期刊：Journal of Medicinal Chemistry, 页码：7532-7548 , 文章类型： Article，,卷期：2010年53-21] In the search for potent ligands at the benzodiazepine site on the GABA(A) receptor, new fluoro derivatives of the pyrazolo[5,1-c][1,2,4]benzotriazine system were synthesized to evaluate the importance of the introductio...