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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26条记录   Discovery of a Novel Alpha-7 Nicotinic Acetylcholine Receptor Agonist Series and Characterization of the Potent, Selective, and Orally Efficacious Agonist 5-(4-Acetyl[1,4]diazepan-1-yl)pentanoic Acid [5-(4-Methoxyphenyl)-1H-pyrazol-3-yl] Amide (SEN15924, WAY-361789) [作者：ZANALETTI RICCARDO; BETTINETTI LAURA; CASTALDO CRISTIANA; COCCONCELLI GIUSEPPE; COMERY THOMAS; DUNLOP JOHN; GAVIRAGHI GIOVANNI; GHIRON CHIARA; HAYDAR SIMON N; JOW FLORA; MACCARI LAURA; MICCO IOLANDA; NENCINI ARIANNA; SCALI CARLA; TURLIZZI ELISA; VALACCHIT MICHELA,期刊：Journal of Medicinal Chemistry, 页码：4806-4823 , 文章类型： Article，,卷期：2012年55-10] Alpha-7 nicotinic acetylcholine receptors (alpha 7 nAChR) are implicated in the modulation of many cognitive functions such as attention, working memory, and episodic memory. For this reason, alpha 7 nAChR agonists repre... N-(2-Oxo-3-oxetanyl)carbamic Acid Esters as N-Acylethanolamine Acid Amidase Inhibitors: Synthesis and Structure-Activity and Structure-Property Relationships [作者：DURANTI ANDREA; TONTINI ANDREA; ANTONIETTI FRANCESCA; VACONDIO FEDERICA; FIONI ALESSANDRO; SILVA CLAUDIA; LODOLA ALESSIO; RIVARA SILVIA; SOLORZANO CARLOS; PIOMELLI DANIELE; TARZIA GIORGIO; MOR MARCO,期刊：Journal of Medicinal Chemistry, 页码：4824-4836 , 文章类型： Article，,卷期：2012年55-10] The beta-lactone ring of N-(2-oxo-3-oxetanypamides, a class of N-acylethanolamine acid amidase (NAAA) inhibitors endowed with anti-inflammatory properties, is responsible for both NAAA inhibition and low compound stabili... A New Class of Highly Potent Matrix Metalloproteinase Inhibitors Based on Triazole-Substituted Hydroxamates: (Radio)Synthesis and in Vitro and First in Vivo Evaluation [作者：HUGENBERG VERENA; BREYHOLZ HANSJOERG; RIEMANN BURKHARD; HERMANN SVEN; SCHOBER OTMAR; SCHAEFERS MICHAEL; GANGADHARMATH UMESH; MOCHARLA VANI; KOLB HARTMUTH; WALSH JOSEPH; ZHANG WEI; KOPKA KLAUS; WAGNER STEFAN,期刊：Journal of Medicinal Chemistry, 页码：4714-4727 , 文章类型： Article，,卷期：2012年55-10] In vivo imaging of MMPs is of great (pre)clinical interest and can potentially be realized with modern three-dimensional and noninvasive in vivo molecular imaging techniques such as positron emission tomography (PET). Co... Discovery of Pyrroloaminopyrazoles as Novel PAK Inhibitors [作者：GUO CHUANGXING; MCALPINE INDRAWAN; ZHANG JUNHU; KNIGHTON DANIEL D; KEPHART SUSAN; JOHNSON M CATHERINE; LI HAITAO; BOUZIDA DJAMAL; YANG ANLE; DONG LIMING; MARAKOVITS JOSEPH; TIKHE JAYASHREE; RICHARDSON PAUL; GUO LISA C; KANIA ROBERT; EDWARDS MARTIN P; KRAYNOV EUGENIA; CHRISTENSEN JAMES; PIRAINO JOSEPH; LEE JOSEPH; DAGOSTINO ELEANOR; DELCARMEN CHRISTINE; DENG YALI; SMEAL TOD; MURRAY BRION W,期刊：Journal of Medicinal Chemistry, 页码：4728-4739 , 文章类型： Article，,卷期：2012年55-10] The P21-activated kinases (PAK) are emerging antitumor therapeutic targets. In this paper, we describe the discovery of potent PAK inhibitors guided by structure-based drug design. In addition, the efflux of the pyrrolop... Classification of Inhibitors of Hepatic Organic Anion Transporting Polypeptides (OATPs): Influence of Protein Expression on Drug - Drug Interactions [作者：KARLGREN MARIA; VILDHEDE ANNA; NORINDER ULF; WISNIEWSKI JACEK R; KIMOTO EMI; LAI YURONG; HAGLUND ULF; ARTURSSON PER,期刊：Journal of Medicinal Chemistry, 页码：4740-4763 , 文章类型： Article，,卷期：2012年55-10] The hepatic organic anion transporting polypeptides (OATPs) influence the pharmacokinetics of several drug classes and are involved in many clinical drug-drug interactions. Predicting potential interactions with OATPs is... Design, Synthesis, and Antiviral Activity of Entry Inhibitors That Target the CD4-Binding Site of HIV-1 [作者：CURRELI FRANCESCA; CHOUDHURY SPREEHA; PYATKIN ILYA; ZAGORODNIKOV VICTOR P; BULAY ANNA KHULIANOVA; ALTIERI ANDREA; DO KWON YOUNG; KWONG PETER D; DEBNATH ASIM K,期刊：Journal of Medicinal Chemistry, 页码：4764-4775 , 文章类型： Article，,卷期：2012年55-10] The CD4 binding site on HIV-1 gp120 has been validated as a drug target to prevent HIV-1 entry to cells. Previously, we identified two small molecule inhibitors consisting of a 2,2,6,6-tetramethylpiperidine ring linked b... Rapid Identification of a Novel Small Molecule Phosphodiesterase 10A (PDE10A) Tracer [作者：HU ESSA; MA JI; BIORN CHRISTOPHER; LESTERZEINER DIANNA; CHO ROBERT; RUMFELT SHANNON; KUNZ ROXANNE K; NIXEY THOMAS; MICHELSEN KLAUS; MILLER SILKE; SHI JIANXIA; WONG JAMIE; DELLA PUPPA GERALDINE HILL; ABLE JESSICA; TALREJA SANTOSH; HWANG DAHREN; HITCHCOCK STEPHEN A; PORTER AMY; IMMKE DAVID; ALLEN JENNIFER R; TREANOR JAMES; CHEN HANG,期刊：Journal of Medicinal Chemistry, 页码：4776-4787 , 文章类型： Article，,卷期：2012年55-10] A radiolabeled tracer for imaging therapeutic targets in the brain is a valuable tool for lead optimization in CNS drug discovery and for dose selection in clinical development. We report the rapid identification of a no... Discovery and Optimization of New Benzimidazole- and Benzoxazole-Pyrimidone Selective PI3K beta Inhibitors for the Treatment of Phosphatase and TENsin homologue (PTEN)-Deficient Cancers [作者：CERTAL VICTOR; HALLEY FRANK; VIRONEODDOS ANGELA; DELORME CECILE; KARLSSON ANDREAS; RAK ALEXEY; THOMPSON FABIENNE; FILOCHEROMME BRUNO; ELAHMAD YOUSSEF; CARRY JEANCHRISTOPHE; ABECASSIS PIERREYVES; LEJEUNE PASCALE; VINCENT LOIC; BONNEVAUX HELENE; NICOLAS JEANPAUL; BERTRAND THOMAS; MARQUETTE JEANPIERRE; MICHOT NADINE; BENARD TSIALA; BELOW PETER; VADE ISABELLE; CHATREAUX FABIENNE; LEBOURG GILES; PILORGE FABIENNE; ANGOUILLANTBONIFACE ODILE; LOUBOUTIN AUDREY; LENGAUER CHRISTOPH; SCHIO LAURENT,期刊：Journal of Medicinal Chemistry, 页码：4788-4805 , 文章类型： Article，,卷期：2012年55-10] Most of the phosphoinositide-3 kinase (PI3K) kinase inhibitors currently in clinical trials for cancer treatment exhibit pan PI3K isoform profiles. Single PI3K isoforms differentially control tumorigenesis, and PI3K beta... Synthesis, Chemical Reactivity as Michael Acceptors, and Biological Potency of Monocyclic Cyanoenones, Novel and Highly Potent Anti-inflammatory and Cytoprotective Agents [作者：ZHENG SUQING; LAXMI Y R SANTOSH; DAVID EMILIE; DINKOYAKOSTOVA ALBENA T; SHIAVONI KATHERINE H; REN YANQING; ZHENG YING; TREVINO ISAAC; BUMEISTER RONALD; OJIMA IWAO; WIGLEY W CHRISTIAN; BLISKA JAMES B; MIERKE DALE F; HONDA TADASHI,期刊：Journal of Medicinal Chemistry, 页码：4837-4846 , 文章类型： Article，,卷期：2012年55-10] Novel monocyclic cyanoenones examined to date display unique features regarding chemical reactivity as Michael acceptors and biological potency. Remarkably, in some biological assays, the simple structure is more potent ... Structure-Guided Design of A(3) Adenosine Receptor-Selective Nucleosides: Combination of 2-Arylethynyl and Bicyclo[3.1.0]hexane Substitutions [作者：TOSH DILIP K; DEFLORIAN FRANCESCA; PHAN KHAI; GAO ZHANGUO; WAN TINA C; GIZEWSKI ELIZABETH; AUCHAMPACH JOHN A; JACOBSON KENNETH A,期刊：Journal of Medicinal Chemistry, 页码：4847-4860 , 文章类型： Article，,卷期：2012年55-10] (N)-Methanocarba adenosine 5'-methyluronamides containing known A(3) AR (adenosine receptor)enhancing modifications, i.e., 2-(arylethynyl)adenine and N-6-methyl or N-6-(3-substituted-benzyl), were nanomolar full agonists... Synthesis and Biological Evaluation of Fatty Acyl Ester Derivatives of (-)-2 ',3 '-Dideoxy-3 '-thiacytidine [作者：AGARWAL HITESH K; CHHIKARA BHUPENDER S; HANLEY MICHAEL J; YE GUOFENG; DONCEL GUSTAVO F; PARANG KEYKAVOUS,期刊：Journal of Medicinal Chemistry, 页码：4861-4871 , 文章类型： Article，,卷期：2012年55-10] A number of fatty acyl derivatives of (-)-2',3'-dideoxy-3'-thiacytidine (lamivudine, 3TC, 1) were synthesized and evaluated for their anti-HIV activity. The monosubstituted 5'-O-fatty acyl derivatives of 3TC (EC50 = 0.2-... Preparation of 3-Substituted-1-Isopropyl-1H-pyrazolo[3,4-d]pyrimidin-4-amines as RET Kinase Inhibitors [作者：DINER PETER; ALAO JOHN P; SODERLUND JOHAN; SUNNERHAGEN PER; GROTLI MORTEN,期刊：Journal of Medicinal Chemistry, 页码：4872-4876 , 文章类型： Article，,卷期：2012年55-10] A series of 3-substituted-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-4-amines have been designed, synthesized, and evaluated as RET protein kinase inhibitors. On the basis of docking results, a small library of pyrazolopyri... Modern Phenotypic Drug Discovery Is a Viable, Neoclassic Pharma Strategy [作者：LEE JONATHAN A; UHLIK MARK T; MOXHAM CHRISTOPHER M; TOMANDL DIRK; SALL DANIEL J,期刊：Journal of Medicinal Chemistry, 页码：4527-4538 , 文章类型： Article，,卷期：2012年55-10] Bruton's Tyrosine Kinase Inhibitors: Approaches to Potent and Selective Inhibition, Preclinical and Clinical Evaluation for Inflammatory Diseases and B Cell Malignancies [作者：LOU YAN; OWENS TIMOTHY D; KUGLSTATTER ANDREAS; KONDRU RAMA K; GOLDSTEIN DAVID M,期刊：Journal of Medicinal Chemistry, 页码：4539-4550 , 文章类型： Article，,卷期：2012年55-10] Flavone-Based Novel Antidiabetic and Antidyslipidemic Agents [作者：VERMA ALOK K; SINGH HIMANSHU; SATYANARAYANA MAVURAPU; SRIVASTAVA SWAYAM P; TIWARI PRITI; SINGH AMAR B; DWIVEDI ANIL K; SINGH SHIO K; SRIVASTAVA MUKESH; NATH CHANDISHWAR; RAGHUBIR RAM; SRIVASTAVA ARVIND K; PRATAP RAM,期刊：Journal of Medicinal Chemistry, 页码：4551-4567 , 文章类型： Article，,卷期：2012年55-10] The hybrid congeners 62-90 of 6- and 7-hydroxyflavones with aminopropanol have been synthesized and evaluated for their antidiabetic activity in sucrose-challenged low-dosed streptozotocin (STZ)-induced diabetic rats and... Anti-inflammatory Active Gold(I) Complexes Involving 6-Substituted-Purine Derivatives [作者：TRAVNICEK ZDENEK; STARHA PAVEL; VANCO JAN; SILHA TAMAS; HOSEK JAN; SUCHY PAVEL JR; PRAZANOVA GABRIELA,期刊：Journal of Medicinal Chemistry, 页码：4568-4579 , 文章类型： Article，,卷期：2012年55-10] The gold(I) complexes of the general formula [Au(L-n)(PPh3)]center dot xH(2)O (1-8; n = 1-8 and x = 0-1.5), where L-n stands for a deprotonated form of the benzyl-substituted derivatives of 6-benzylaminopurine, were prep...