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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49条记录   Discovery and Characterization of 6-{4[3-(R)-2-Methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, Irdabisant): A Potent, Selective Histamine H(3) Receptor Inverse Agonist [作者：HUDKINS ROBERT L; RADDATZ RITA; TAO MING; MATHIASEN JOANNE R; AIMONE LISA D; BECKNELL NADINE C; PROUTY CATHERINE P; KNUTSEN LARS J S; YAZDANIAN MEHRAN; MOACHON GILBERT; ATOR MARK A; MALLAMO JOHN P; MARINO MICHAEL J; BACON EDWARD R; WILLIAMS MICHAEL,期刊：Journal of Medicinal Chemistry, 页码：4781-4792 , 文章类型： Article，,卷期：2011年54-13] Optimization of a novel series of pyridazin-3-one histamine H(3) receptor (H(3)R) antagonists/inverse agonists identified 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (8a, CEP-26401; irdabisant)... Selective Kainate Receptor (GluK1) Ligands Structurally Based upon 1H-Cyclopentapyrimidin-2,4(1H,3H)-dione: Synthesis, Molecular Modeling, and Pharmacological and Biostructural Characterization [作者：VENSKUTONYTE RAMINTA; BUTINI STEFANIA; COCCONE SALVATORE SANNA; GEMMA SANDRA; BRINDISI MARGHERITA; KUMAR VINOD; GUARINO EGERIA; MARAMAI SAMUELE; VALENTI SALVATORE; AMIR AHMAD; VALADES ELENA ANTON; FRYDENVANG KARLA; KASTRUP JETTE S; NOVELLINO ETTORE; CAMPIANI GIUSEPPE; PICKERING DARRYL S,期刊：Journal of Medicinal Chemistry, 页码：4793-4805 , 文章类型： Article，,卷期：2011年54-13] The physiological function of kainate receptors (GluK1-GluK5) in the central nervous system is not fully understood yet. With the aim of developing potent and selective GluK1 ligands, we have synthesized a series of new ... Structure-Activity Relationships of a Series of Analogues of the RFamide-Related Peptide 26RFa [作者：LE MAREC OLIVIER; NEVEU CINDY; LEFRANC BENJAMIN; DUBESSY CHRISTOPHE; BOUTIN JEAN A; DOREGO JEANCLAUDE; COSTENTIN JEAN; TONON MARIECHRISTINE; TENASEMPERE MANUEL; VAUDRY HUBERT; LEPRINCE JEROME,期刊：Journal of Medicinal Chemistry, 页码：4806-4814 , 文章类型： Article，,卷期：2011年54-13] 26RFa is a new member of the RFamide peptide family that has been identified as the endogenous ligand of the orphan GPCR GPR103. As the C-terminal heptapeptide (26RFa((20-26))) mimics the action of the native peptide on ... Primary Amino Acid Derivatives: Compounds with Anticonvulsant and Neuropathic Pain Protection Activities [作者：KING AMBER M; SALOME CHRISTOPHE; DINSMORE JASON; SALOMEGROSJEAN ELISE; DE RYCK MARC; KAMINSKI RAFAL; VALADE ANNE; KOHN HAROLD,期刊：Journal of Medicinal Chemistry, 页码：4815-4830 , 文章类型： Article，,卷期：2011年54-13] Pharmacological management remains the primary method to treat epilepsy and neuropathic pain. We have advanced a novel class of anticonvulsants termed functionalized amino acids (FAAs). In this study, we examine FAA deri... Binding Inhibitors of the Bacterial Sliding Clamp by Design [作者：WIJFFELS GENE; JOHNSON WYNONA M; OAKLEY AARON J; TURNER KATHLEEN; EPA V CHANDANA; BRISCOE SUSAN J; POLLEY MITCHELL; LIEPA ANDRIS J; HOFMANN ALBERT; BUCHARDT JENS; CHRISTENSEN CASPAR; PROSSELKOV PAVEL; DALRYMPLE BRIAN P; ALEWOOD PAUL F; JENNINGS PHILIP A; DIXON NICHOLAS E; WINKLER DAVID A,期刊：Journal of Medicinal Chemistry, 页码：4831-4838 , 文章类型： Article，,卷期：2011年54-13] The bacterial replisome is a target for the development of new antibiotics to combat drug resistant strains. The beta(2) sliding clamp is an essential component of the replicative machinery, providing a platform for recr... Structure-Activity Relationships of Carboline and Carbazole Derivatives as a Novel Class of ATP-Competitive Kinesin Spindle Protein Inhibitors [作者：TAKEUCHI TOMOKI; OISHI SHINYA; WATANABE TOSHIAKI; OHNO HIROAKI; SAWADA JUNICHI; MATSUNO KENJI; ASAI AKIRA; ASADA NAOYA; KITAURA KAZUO; FUJII NOBUTAKA,期刊：Journal of Medicinal Chemistry, 页码：4839-4846 , 文章类型： Article，,卷期：2011年54-13] The kinesin spindle protein (KSP) is a mitotic kinesin involved in the establishment of a functional bipolar mitotic spindle during cell division. It is considered to be an attractive target for cancer chemotherapy with ... Synthesis and Evaluation of 5-Substituted 2 '-deoxyuridine Monophosphate Analogues As Inhibitors of Flavin-Dependent Thymidylate Synthase in Mycobacterium tuberculosis [作者：KOGLER MARTIN; VANDERHOYDONCK BART; DE JONGHE STEVEN; ROZENSKI JEF; VAN BELLE KRISTIEN; HERMAN JEAN; LOUAT THIERRY; PARCHINA ANASTASIA; SIBLEY CAROL; LESCRINIER EVELINE; HERDEWIJN PIET,期刊：Journal of Medicinal Chemistry, 页码：4847-4862 , 文章类型： Article，,卷期：2011年54-13] A series of 5-substituted 2'-deoxyuridine monophosphate analogues has been synthesized and evaluated as potential inhibitors of mycobacterial ThyX, a novel flavin-dependent thymidylate synthase in Mycobacterium tuberculo... Structure-Activity Relationships of C-17-Substituted Estratriene-3-O-sulfamates as Anticancer Agents [作者：JOURDAN FABRICE; LEESE MATHEW P; DOHLE WOLFGANG; FERRANDIS ERIC; NEWMAN SIMON P; CHANDER SURINDER; PUROHIT ATUL; POTTER BARRY V L,期刊：Journal of Medicinal Chemistry, 页码：4863-4879 , 文章类型： Article，,卷期：2011年54-13] The synthesis and antiproliferative activities of analogues of 2-substituted estradiol-3,17-O,O-bis-sulfamates (E2bisMATEs) are discussed. Modifications of the C-17 substituent confirm that an H-bond acceptor is essentia... Biphenyl-Substituted Oxazolidinones as Cholesteryl Ester Transfer Protein Inhibitors: Modifications of the Oxazolidinone Ring Leading to the Discovery of Anacetrapib [作者：SMITH CAMERON J; ALI AMJAD; HAMMOND MILTON L; LI HONG; LU ZHIJIAN; NAPOLITANO JOANN; TAYLOR GAYLE E; THOMPSON CHRISTOPHER F; ANDERSON MATT S; CHEN YING; EVELAND SUZANNE S; GUO QIU; HYLAND SHERYL A; MILOT DENISE P; SPARROW CARL P; WRIGHT SAMUEL D; CUMISKEY ANNEMARIE; LATHAM MELANIE; PETERSON LAURENCE B; ROSA RAY; PIVNICHNY JAMES V; TONG XINCHUN; XU SUOYU S; SINCLAIR PETER J,期刊：Journal of Medicinal Chemistry, 页码：4880-4895 , 文章类型： Article，,卷期：2011年54-13] The development of the structure-activity studies leading to the discovery of anacetrapib is described. These studies focused on varying the substitution of the oxazolidinone ring of the 5-aryloxazolidinone system. Speci... Bivalent Dopamine D(2) Receptor Ligands: Synthesis and Binding Properties [作者：KUEHHORN JULIA; HUEBNER HARALD; GMEINER PETER,期刊：Journal of Medicinal Chemistry, 页码：4896-4903 , 文章类型： Article，,卷期：2011年54-13] Dopamine D(2) receptor homodimers might be of e particular importance in the pathophysiology of schizophrenia and, thus, serve as promising target proteins for the discovery of atypical antipsychotics. A highly attractiv... Cyclic Nucleotide-Gated Channel Block by Hydrolysis-Resistant Tetracaine Derivatives [作者：ANDRADE ADRIANA L; MELICH KENNETH; WHATLEY G GREGORY; KIRK SARAH R; KARPEN JEFFREY W,期刊：Journal of Medicinal Chemistry, 页码：4904-4912 , 文章类型： Article，,卷期：2011年54-13] To meet a pressing need for better cyclic nucleotide-gated (CNG) channel antagonists, we have increased the biological stability of tetracaine-based blockers by synthesizing amide and thioamide linkage substitutions of t... A New Class of Phenazines with Activity against a Chloroquine Resistant Plasmodium falciparum Strain and Antimicrobial Activity [作者：HUSSAIN HIDAYAT; SPECHT SABINE; SARITE SALEM R; SAEFTEL MICHAEL; HOERAUF ACHIM; SCHULZ BARBARA; KROHN KARSTEN,期刊：Journal of Medicinal Chemistry, 页码：4913-4917 , 文章类型： Article，,卷期：2011年54-13] New phenazines were synthesized by oxygenation of 1- and 2-naphthol with transition metal peroxo complexes and in situ reaction with 1,2-diamines. The title compounds were evaluated for in vitro antimalarial activity aga... Synthesis of New Vitamin K Analogues as Steroid and Xenobiotic Receptor (SXR) Agonists: Insights into the Biological Role of the Side Chain Part of Vitamin K [作者：SUHARA YOSHITOMO; WATANABE MASATO; MOTOYOSHI SAYAKA; NAKAGAWA KIMIE; WADA AKIMORI; TAKEDA KAZUYOSHI; TAKAHASHI KAZUHIKO; TOKIWA HIROAKI; OKANO TOSHIO,期刊：Journal of Medicinal Chemistry, 页码：4918-4922 , 文章类型： Article，,卷期：2011年54-13] Vitamin K(2) has been demonstrated to induce gene expression related to bone formation through a nuclear steroid and xenobiotic receptor (SXR). We synthesized new vitamin K analogues with the same isoprene side chains sy... Synthesis and Evaluation of Diarylthiazole Derivatives That Inhibit Activation of Sterol Regulatory Element-Binding Proteins [作者：KAMISUKI SHINJI; SHIRAKAWA TAKASHI; KUGIMIYA AKIRA; ABUELHEIGA LUTFI; CHOO HEAYOUNG PARK; YAMADA KOHEI; SHIMOGAWA HIROKI; WAKIL SALIH J; UESUGI MOTONARI,期刊：Journal of Medicinal Chemistry, 页码：4923-4927 , 文章类型： Article，,卷期：2011年54-13] Fatostatin, a recently discovered small molecule that inhibits activation of sterol regulatory element-binding protein (SREBP), blocks biosynthesis and accumulation of fat in obese mice. We synthesized and evaluated a se... Novel 3,5-Bis(bromohydroxybenzylidene)piperidin-4-ones as Coactivator-Associated Arginine Methyltransferase 1 Inhibitors: Enzyme Selectivity and Cellular Activity [作者：CHENG DONGHANG; VALENTE SERGIO; CASTELLANO SABRINA; SBARDELLA GIANLUCA; DI SANTO ROBERTO; COSTI ROBERTA; BEDFORD MARK T; MAI ANTONELLO,期刊：Journal of Medicinal Chemistry, 页码：4928-4932 , 文章类型： Article，,卷期：2011年54-13] Coactivator-associated arginine methyltransferase 1 (CARM1) represents a valuable target for hormone-dependent tumors such as prostate and breast cancers. Here we report the enzyme and cellular characterization of the 1-... Progress in Structure Based Drug Design for G Protein-Coupled Receptors [作者：CONGREVE MILES; LANGMEAD CHRISTOPHER J; MASON JONATHAN S; MARSHALL FIONA H,期刊：Journal of Medicinal Chemistry, 页码：4283-4311 , 文章类型： Editorial Material，,卷期：2011年54-13]