个性化文献订阅>文章检索

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21条记录   Discovery of 1-(3-{2-[4-(2-Methyl-5-quinolinyl)-1-piperazinyl]ethyl}phenyl)-2-imidazolidinone (GSK163090), a Potent, Selective, and Orally Active 5-HT1A/B/D Receptor Antagonist [作者：LESLIE COLIN P; BIAGETTI MATTEO; BISON SILVIA; BROMIDGE STEVEN M; DI FABIO ROMANO; DONATI DANIELE; FALCHI ALESSANDRO; GARNIER MARTINE J; JAXACHAMIEC ALBERT; MANCHEE GARY; MERLO GIANCARLO; PIZZI DOMENICA A; STASI LUIGI P; TIBASCO JESSICA; VONG ANTONIO; WARD SIMON E; ZONZINI LAURA,期刊：Journal of Medicinal Chemistry, 页码：8228-8240 , 文章类型： Article，,卷期：2010年53-23] In an effort to identify selective drug like pan-antagonists of the 5-HT1 autoreceptors, studies were conducted to elaborate a previously reported dual acting 5-HT1 antagonist/SSRI structure. A novel series of compounds ... Dimethyl-diphenyl-propanamide Derivatives As Nonsteroidal Dissociated Glucocorticoid Receptor Agonists [作者：YANG BINGWEI V; WEINSTEIN DAVID S; DOWEYKO LIDIA M; GONG HUA; VACCARO WAYNE; HUYNH TRAM; XIAO HAIYUN; DOWEYKO ARTHUR M; MCKAY LORRAINE; HOLLOWAY DEBORAH A; SOMERVILLE JOHN E; HABTE SIUM; CUNNINGHAM MARK; MCMAHON MICHELE; TOWNSEND ROBERT; SHUSTER DAVID; DODD JOHN H; NADLER STEVEN G; BARRISH JOEL C,期刊：Journal of Medicinal Chemistry, 页码：8241-8251 , 文章类型： Article，,卷期：2010年53-23] A series of 2,2-dimethyl-3,3-diphenyl-propanamides as novel glucocorticoid receptor modulators is reported. SAR exploration led to the identification of 4-hydroxyphenyl propanamide derivatives displaying good agonist act... Hydroxycoumarin Derivatives: Novel and Potent alpha-Glucosidase Inhibitors [作者：SHEN QIONG; SHAO JIALIANG; PENG QUAN; ZHANG WANJIN; MA LIN; CHAN ALBERT S C; GU LIANQUAN,期刊：Journal of Medicinal Chemistry, 页码：8252-8259 , 文章类型： Article，,卷期：2010年53-23] A novel class of hydroxycoumarin derivatives were found to be potent alpha-glucosidase inhibitors. Their syntheses were reported and the structure-activity relationship was established. Kinetic enzymatic assays indicated... Synthesis and Identification of New 4-Arylidene Curcumin Analogues as Potential Anticancer Agents Targeting Nuclear Factor-kappa B Signaling Pathway [作者：QIU XU; DU YUHONG; LOU BIN; ZUO YINGLIN; SHAO WEIYAN; HUO YINGPENG; HUANG JIANING; YU YANJUN; ZHOU BINHUA; DU JUN; FU HAIAN; BU XIANZHANG,期刊：Journal of Medicinal Chemistry, 页码：8260-8273 , 文章类型： Article，,卷期：2010年53-23] A series of curcumin analogues including new 4-arylidene curcumin analogues (4-arylidene-1,7-bisarylhepta-1,6-diene-3,5-diones) were synthesized. Cell growth inhibition assays revealed that most 4-arylidene curcumin anal... A Synthetic 7,8-Dihydroxyflavone Derivative Promotes Neurogenesis and Exhibits Potent Antidepressant Effect [作者：LIU XIA; CHAN CHIBUN; JANG SUNGWUK; PRADOLDEJ SOMPOL; HUANG JUNJIAN; HE KUNYAN; PHUN LIEN H; FRANCE STEFAN; XIAO GE; JIA YONGHUI; LUO HONGBO R; YE KEQIANG,期刊：Journal of Medicinal Chemistry, 页码：8274-8286 , 文章类型： Article，,卷期：2010年53-23] 7,8-Dihydroxyflavone is a recently identified small molecular tropomyosin-receptor-kinase B (TrkB) agonist. Our preliminary structural activity relationship (SAR) study showed that the 7,8-dihydroxy groups are essential ... Design, Synthesis, and Evaluation of Diarylpyridines and Diarylanilines as Potent Non-nucleoside HIV-1 Reverse Transcriptase Inhibitors [作者：TIAN XINGTAO; QIN BINGJIE; WU ZHIYUAN; WANG XIAOFENG; LU HONG; MORRISNATSCHKE SUSAN L; CHEN CHIN HO; JIANG SHIBO; LEE KUOHSIUNG; XIE LAN,期刊：Journal of Medicinal Chemistry, 页码：8287-8297 , 文章类型： Article，,卷期：2010年53-23] On the basis of the structures and activities of our previously identified non-nucleoside reverse transcriptase inhibitors (NNRTIs), we designed and synthesized two sets of derivatives, diarylpyridines (A) and diarylanil... 1-(5-Carboxyindol-1-yl)propan-2-one Inhibitors of Human Cytosolic Phospholipase A(2)alpha.: Effect of Substituents in Position 3 of the Indole Scaffold on Inhibitory Potency, Metabolic Stability, Solubility, and Bioavailability [作者：BOVENS STEFANIE; ELFRINGHOFF ALWINE SCHULZE; KAPTUR MARTINA; REINHARDT DIRK; SCHAEFERS MICHAEL; LEHR MATTHIAS,期刊：Journal of Medicinal Chemistry, 页码：8298-8308 , 文章类型： Article，,卷期：2010年53-23] Indole-5-carboxylic acids with 3-aryloxy-2-oxopropyl residues in position I have been found to be potent inhibitors of human cytosolic phospholipase A(2)alpha (cPLA(2)alpha). In the course of structure-activity relations... Configuration of the 5 '-Methyl Group Modulates the Biophysical and Biological Properties of Locked Nucleic Acid (LNA) Oligonucleotides [作者：SETH PUNIT P; ALLERSON CHARLES R; SIWKOWSKI ANDREW; VASQUEZ GUILLERMO; BERDEJA ANDRES; MIGAWA MICHAEL T; GAUS HANS; PRAKASH THAZHA P; BHAT BALKRISHEN; SWAYZE ERIC E,期刊：Journal of Medicinal Chemistry, 页码：8309-8318 , 文章类型： Article，,卷期：2010年53-23] As part of a program aimed at exploring the structure activity relationships of 2',4'-bridged nucleic acid (BNA) containing antisense oligonucleotides (ASOs), we report the synthesis and biophysical and biological proper... Identification of the Spiro(oxindole-3,3 '-thiazolidine)-Based Derivatives as Potential p53 Activity Modulators [作者：GOMEZMONTERREY ISABEL; BERTAMINO ALESSIA; PORTA AMALIA; CAROTENUTO ALFONSO; MUSELLA SIMONA; AQUINO CLAUDIO; GRANATA ILARIA; SALA MARINA; BRANCACCIO DIEGO; PICONE DELIA; ERCOLE CARMINE; STIUSO PAOLA; CAMPIGLIA PIETRO; GRIECO PAOLO; IANELLI PIO; MARESCA BRUNO; NOVELLINO ETTORE,期刊：Journal of Medicinal Chemistry, 页码：8319-8329 , 文章类型： Article，,卷期：2010年53-23] Here, we report the design of new analogues of spirooxoindolepyrrolidine nucleus as modulators of p53 activity. Compounds (3R,7aR)-6(4-chlorobenzyl)-1H-spiro[imidazo[1,5-c]thiazole-3,3'-indolin e]-2',5,7(6H,7aH)-trione (... Acetic Acid Derivatives of 3,4-Dihydro-2H-1,2,4-benzothiadiazine 1,1-Dioxide as a Novel Class of Potent Aldose Reductase Inhibitors [作者：CHEN XIN; ZHU CHANGJIN; GUO FAN; QIU XIAOWEI; YANG YANCHUN; ZHANG SHUZHEN; HE MINLAN; PARVEEN SHAGUFTA; JING CHAOJUN; LI YAN; MA BING,期刊：Journal of Medicinal Chemistry, 页码：8330-8344 , 文章类型： Article，,卷期：2010年53-23] A series of novel benzothiadiazine 1,1-dioxide derivatives were synthesized and tested for their inhibitory activity against aldose reductase. Of these derivatives, 17 compounds, having a substituted N2-benzyl group and ... Nicotinic Acetylcholine Receptor Efficacy and Pharmacological Properties of 3-(Substituted phenyl)-2 beta-substituted Tropanes [作者：CARROLL F IVY; BLOUGH BRUCE E; MASCARELLA S WAYNE; NAVARRO HERNAN A; EATON J BREK; LUKAS RONALD J; DAMAJ M IMAD,期刊：Journal of Medicinal Chemistry, 页码：8345-8353 , 文章类型： Article，,卷期：2010年53-23] There is a need for different and better aids to tobacco product use cessation. Useful smoking cessation aids, bupropion (2) and varenicline (3), share some chemical features with 3-phenyltropanes (4), which have promise... Biostructural and Pharmacological Studies of Bicyclic Analogues of the 3-Isoxazolol Glutamate Receptor Agonist Ibotenic Acid [作者：FRYDENVANG KARLA; PICKERING DARRYL S; GREENWOOD JEREMY R; KROGSGAARDLARSEN NIELS; BREHM LOTTE; NIELSEN BIRGITTE; VOGENSEN STINE B; HALD HELLE; KASTRUP JETTE S; KROGSGAARDLARSEN POVL; CLAUSEN RASMUS P,期刊：Journal of Medicinal Chemistry, 页码：8354-8361 , 文章类型： Article，,卷期：2010年53-23] We describe an improved synthesis and detailed pharmacological characterization of the conformationally restricted analogue of the naturally occurring nonselective glutamate receptor agonist ibotenic acid (RS)-3-hydroxy-... Novel Small Molecule Inhibitors of MDR Mycobacterium tuberculosis by NMR Fragment Screening of Antigen 85C [作者：SCHEICH CHRISTOPH; PUETTER VERA; SCHADE MARKUS,期刊：Journal of Medicinal Chemistry, 页码：8362-8367 , 文章类型： Article，,卷期：2010年53-23] Protein target-based discovery of novel antibiotics has been largely unsuccessful despite rich genome information. Particularly in need are new antibiotics for tuberculosis, which kills 1.6 million people annually and sh... Design, Synthesis, and Structure-Activity Relationships of 3-Ethynyl-1H-indazoles as Inhibitors of the Phosphatidylintositol 3-Kinase Signaling Pathway [作者：BARILE ELISA; DE SURYA K; CARLSON COBY B; CHEN VIDA; KNUTZEN CHRISTINE; RIELMEHAN MEGAN; YANG LI; DAHL RUSSELL; CHIANG GARY; PELLECCHIA MAURIZIO,期刊：Journal of Medicinal Chemistry, 页码：8368-8375 , 文章类型： Article，,卷期：2010年53-23] A new series of 3-ethynyl-1H-indazoles has been synthesized and evaluated in both biochemical and cell-based assays as potential kinase inhibitors. Interestingly, a selected group of compounds identified from this series... Incorporation of Piperazino Functionality into 1,3-Disubstituted Urea as the Tertiary Pharmacophore Affording Potent Inhibitors of Soluble Epoxide Hydrolase with Improved Pharmacokinetic Properties [作者：HUANG SHAOXU; LI HUIYUAN; LIU JUNYAN; MORISSEAU CHRISTOPHE; HAMMOCK BRUCE D; LONG YAQIU,期刊：Journal of Medicinal Chemistry, 页码：8376-8386 , 文章类型： Article，,卷期：2010年53-23] The inhibition of the mammalian soluble epoxide hydrolase (sEH) is a promising new therapy in the treatment of hypertension, inflammation, and other disorders. However, the problems of limited water solubility, high melt... Non-Natural Macrocyclic Inhibitors of Histone Deacetylases: Design, Synthesis, and Activity [作者：AUZZAS LUCIANA; LARSSON ANDREAS; MATERA RICCARDO; BARALDI ANNAMARIA; DESCHENESSIMARD BENOIT; GIANNINI GIUSEPPE; CABRI WALTER; BATTISTUZZI GIANFRANCO; GALLO GRAZIA; CIACCI ANDREA; VESCI LOREDANA; PISANO CLAUDIO; HANESSIAN STEPHEN,期刊：Journal of Medicinal Chemistry, 页码：8387-8399 , 文章类型： Article，,卷期：2010年53-23] Nonpeptidic chiral macrocycles were designed on the basis of an analogue of suberoylanilide hydroxamic acid (2) (SAHA, vorinostat) and evaluated against 11 histone deacetylase (HDAC) isoforms. The identification of criti...