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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37条记录   Discovery, Structure-Activity Relationships, Pharmacokinetics, and Efficacy of Glucokinase Activator (2R)-3-Cyclopentyl-2-(4-methanesulfonylphenyl)-N-thiazol-2-yl-propionamide (RO0281675) [作者：HAYNES NANCYELLEN; CORBETT WENDY L; BIZZARRO FRED T; GUERTIN KEVIN R; HILLIARD DARRYL W; HOLLAND GEORGE W; KESTER ROBERT F; MAHANEY PAIGE E; QI LIDA; SPENCE CHERYL L; TENGI JOHN; DVOROZNIAK MARK T; RAILKAR ARUNA; MATSCHINSKY FRANZ M; GRIPPO JOSEPH F; GRIMSBY JOSEPH; SARABU RAMAKANTH,期刊：Journal of Medicinal Chemistry, 页码：3618-3625 , 文章类型： Article，,卷期：2010年53-9] Glucokinase (GK) is a glucose sensor that couples glucose metabolism to insulin release. The important role of GK in maintaining glucose homeostasis is illustrated in patients with GK mutations. In this publication, iden... Antibacterial Activities of Aminoglycoside Antibiotics-Derived Cationic Amphiphiles. Polyol-Modified Neomycin B-, Kanamycin A-, Amikacin-, and Neamine-Based Amphiphiles with Potent Broad Spectrum Antibacterial Activity [作者：BERA SMRITILEKHA; ZHANEL GEORGE G; SCHWEIZER FRANK,期刊：Journal of Medicinal Chemistry, 页码：3626-3631 , 文章类型： Article，,卷期：2010年53-9] Cationic amphiphiles containing multiple positively charged amino functions define a structurally diverse class of antibacterials with broad-spectrum activity and different modes of action. Oligocationic amphiphiles have... Macrocyclic Pyridyl Polyoxazoles: Selective RNA and DNA G-Quadruplex Ligands as Antitumor Agents [作者：RZUCZEK SUZANNE G; PILCH DANIEL S; LIU ANGELA; LIU LEROY; LAVOIE EDMOND J; RICE JOSEPH E,期刊：Journal of Medicinal Chemistry, 页码：3632-3644 , 文章类型： Article，,卷期：2010年53-9] The synthesis of a series of 24-membered pyridine-containing polyoxazole macrocycles is described. Seventeen new macrocycles were evaluated for cytotoxic activity against RPMI 8402, KB-3, and KB-3 cell lines that overexp... Tetrahydrochromenoimidazoles as Potassium-Competitive Acid Blockers (P-CABs): Structure-Activity Relationship of Their Antisecretory Properties and Their Affinity toward the hERG Channel [作者：PALMER ANDREAS M; CHIESA VITTORIA; SCHMID ANJA; MUENCH GABRIELA; GROBBEL BURKHARD; ZIMMERMANN PETER J; BREHM CHRISTOF; BUHR WILM; SIMON WOLFGANGALEXANDER; KROMER WOLFGANG; POSTIUS STEFAN; VOLZ JUERGEN; HES DIETMAR,期刊：Journal of Medicinal Chemistry, 页码：3645-3674 , 文章类型： Article，,卷期：2010年53-9] Potassium-competitive acid blockers (P-CABs) constitute a new therapeutic option for the treatment of acid-related diseases that are widespread and constitute a significant economical burden. Enantiomerically pure tetrah... The Identification of Indacaterol as an Ultralong-Acting Inhaled beta(2)-Adrenoceptor Agonist [作者：BAUR FRANCOIS; BEATTIE DAVID; BEER DAVID; BENTLEY DAVID; BRADLEY MICHELLE; BRUCE IAN; CHARLTON STEVEN J; CUENOUD BERNARD; ERNST ROLAND; FAIRHURST ROBIN A; FALLER BERNARD; FARR DAVID; KELLER THOMAS; FOZARD JOHN R; FULLERTON JOE; GARMAN SHEILA; HATTO JULIA; HAYDEN CLAIRE; HE HANDAN; HOWES COLIN; JANUS DIANA; JIANG ZHENGJIN; LEWIS CHRISTINE; LOEUILLETRITZLER FREDERIQUE; MOSER HEINZ; REILLY JOHN; STEWARD ALAN; SYKES DAVID; TEDALDI LAUREN; TRIFILIEFF ALEXANDRE; TWEED MORRIS; WATSON SIMON; WISSLER ELKE; WYSS DANIEL,期刊：Journal of Medicinal Chemistry, 页码：3675-3684 , 文章类型： Article，,卷期：2010年53-9] Following a lipophilicity-based hypothesis, an 8-hydroxyquinolinone 2-aminoindan derived series of beta(2)-adrenoceptor agonists have been prepared and evaluated for their potential as inhaled ultralong-acting bronchodil... Development of a New Generation of 4-Aminoquinoline Antimalarial Compounds Using Predictive Pharmacokinetic and Toxicology Models [作者：RAY SUNETRA; MADRID PETER B; CATZ PAUL; LEVALLEY SUSANNA E; FURNISS MICHAEL J; RAUSCH LINDA L; GUY R KIPLIN; DERISI JOSEPH L; IYER LALITHA V; GREEN CAROL E; MIRSALIS JON C,期刊：Journal of Medicinal Chemistry, 页码：3685-3695 , 文章类型： Article，,卷期：2010年53-9] Among the known antimalarial drugs, chloroquine (CQ) and other 4-aminoquinolines have shown high potency and good bioavailability. Yet complications associated with drug resistance necessitate the discovery of effective ... 5,5 '-Substituted Indirubin-3 '-oxime Derivatives as Potent Cyclin-Dependent Kinase Inhibitors with Anticancer Activity [作者：CHOI SOOJEONG; LEE JUNGEUN; JEONG SOONYOUNG; IM ISAK; LEE SODEOK; LEE EUNJIN; LEE SANG KOOK; KWON SEONGMIN; AHN SANGGUN; YOON JUNGHOON; HAN SUNYOUNG; KIM JAEIL; KIM YONGCHUL,期刊：Journal of Medicinal Chemistry, 页码：3696-3706 , 文章类型： Article，,卷期：2010年53-9] To enhance the ability of indirubin derivatives to inhibit CDK2/cyclin E, a target of anticancer agents, we designed and synthesized a new series of indirubin-3'-oxime derivatives with combined substitutions at the 5 and... Mono-, Di-, and Triaryl Substituted Tetrahydropyrans as Cyclooxygenase-2 and Tumor Growth Inhibitors. Synthesis and Biological Evaluation [作者：SINGH PALWINDER; BHARDWAJ ATUL,期刊：Journal of Medicinal Chemistry, 页码：3707-3717 , 文章类型： Article，,卷期：2010年53-9] Rationally designed tetrahydropyrans (THPs) carrying one, two, or three aryl rings and other substituents were synthesized by the allylation of beta-hydroxy ketones followed by iodocyclization. It has been observed that ... Targeting Multiple Chorismate-Utilizing Enzymes with a Single inhibitor: Validation of a Three-Stage Design [作者：ZIEBART KRISTIN T; DIXON SETH M; AVILA BELEM; ELBADRI MOHAMED H; GUGGENHEIM KATHRYN G; KURTH MARK J; TONEY MICHAEL D,期刊：Journal of Medicinal Chemistry, 页码：3718-3729 , 文章类型： Article，,卷期：2010年53-9] Chorismate-utilizing enzymes are attractive antimicrobial drug targets due to their absence in humans and their central role in bacterial survival and virulence. The structural and mechanistic homology of a group of thes... Impact of Nature and Length of Linker Incorporated in Agonists on Toll-Like Receptor 9-Mediated Immune Responses [作者：PUTTA MALLIKARJUNA REDDY; YU DONG; BHAGAT LAKSHMI; WANG DAQING; ZHU FUGANG; KANDIMALLA EKAMBAR R,期刊：Journal of Medicinal Chemistry, 页码：3730-3738 , 文章类型： Article，,卷期：2010年53-9] Oligodeoxynucleotides containing unmethylated CpG motifs act as ligands of Toll-like receptor 9 (TLR9). We previously reported a novel class of TLR9 agonists, referred to as immune-modulatory oligonucleotides (IMOs), in ... Discovery of Brain-Penetrant, Orally Bioavailable Aminothienopyridazine Inhibitors of Tau Aggregation [作者：BALLATORE CARLO; BRUNDEN KURT R; PISCITELLI FRANCESCO; JAMES MICHAEL J; CROWE ALEX; YAO YUEMANG; HYDE EDWARD; TROJANOWSKI JOHN Q; LEE VIRGINIA M Y; SMITH AMOS B III,期刊：Journal of Medicinal Chemistry, 页码：3739-3747 , 文章类型： Article，,卷期：2010年53-9] Agents capable of preventing the misfolding and sequestration of the microtubule-stabilizing protein tau into insoluble fibrillar aggregates hold considerable promise for the prevention and/or treatment of neurodegenerat... Structure-Based Discovery of A(2A) Adenosine Receptor Ligands [作者：CARLSSON JENS; YOO LENA; GAO ZHANGUO; IRWIN JOHN J; SHOICHET BRIAN K; JACOBSON KENNETH A,期刊：Journal of Medicinal Chemistry, 页码：3748-3755 , 文章类型： Article，,卷期：2010年53-9] The recent determination of X-ray structures of pharmacologically relevant GPCRs has made these targets accessible to structure-based ligand discovery. Here we explore whether novel chemotypes may be discovered for the A... Merging the Structural Motifs of Functionalized Amino Acids and alpha-Aminoamides: Compounds with Significant Anticonvulsant Activities [作者：SALOME CHRISTOPHE; SALOMEGROSJEAN ELISE; STABLES JAMES P; KOHNA HAROLD,期刊：Journal of Medicinal Chemistry, 页码：3756-3771 , 文章类型： Article，,卷期：2010年53-9] Functional amino acids (FAAs) and alpha-aminoamides (AAAs) are two classes of antiepileptic drugs (AEDs) that exhibit pronounced anticonvulsant activities. We combined key structural pharmacophores present in FAAs and AA... Pyrazolylthiazole as Delta F508-Cystic Fibrosis Transmembrane Conductance Regulator Correctors with Improved Hydrophilicity Compared to Bithiazoles [作者：YE LONG; KNAPP JOHN M; SANGWUNG PANJAMAPORN; FETTINGER JAMES C; VERKMAN A S; KURTH MARK J,期刊：Journal of Medicinal Chemistry, 页码：3772-3781 , 文章类型： Article，,卷期：2010年53-9] Deletion of phenylalanine residue 508 (Delta F508) in the cystic fibrosis (CF) transmembrane conductance regulator protein (CFTR) is a major cause of CF. Small molecule "correctors" of defective A Delta 508-CFTR cellular... Liposomal Formulation of Retinoids Designed for Enzyme Triggered Release [作者：PEDERSEN PALLE J; ADOLPH SIDSEL K; SUBRAMANIAN ARUN K; AROURI AHMAD; ANDRESEN THOMAS L; MOURITSEN OLE G; MADSEN ROBERT; MADSEN MOGENS W; PETERS GUNTHER H; CLAUSEN MADS H,期刊：Journal of Medicinal Chemistry, 页码：3782-3792 , 文章类型： Article，,卷期：2010年53-9] The design of retinoid phospholipid prodrugs is described based on molecular dynamics simulations and cytotoxicity studies of synthetic retinoid esters. The prodrugs are degradable by secretory phospholipase A(2) IIA and... Function-Oriented Synthesis of Simplified Caprazamycins: Discovery of Oxazolidine-Containing Uridine Derivatives as Antibacterial Agents against Drug-Resistant Bacteria [作者：II KENSUKE; ICHIKAWA SATOSHI; ALDABBAGH BAYAN; BOUHSS AHMED; MATSUDA AKIRA,期刊：Journal of Medicinal Chemistry, 页码：3793-3813 , 文章类型： Article，,卷期：2010年53-9] The rational simplification of the caprazamycin (CPZ) class of nucleoside natural products was carried out to address their molecular complexity. First, analogues 6-8, where the diazepanone ring of the CPZ was removed an...