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13条记录   Efficient Radiosynthesis of 2-[F-18]Fluoroadenosine: A New Route to 2-[F-18]Fluoropurine Nucleosides [作者：MARCHAND PATRICE; LORILLEUX CHRISTOPHE; GILBERT GWENAELLE; GOURAND FABIENNE; SOBRIO FRANCK; PEYRONNET DAMIEN; DHILLY MARTINE; BARRE LOUISA,期刊：ACS Medicinal Chemistry Letters, 页码：240-243 , 文章类型： Article，,卷期：2010年1-6] An efficient method to incorporate the fluorine-18 radionuclide in 2-nitropurine-based nucleosides was developed. The nucleophilic radiofluorination of the labeling precursor with [F-18]KF under aminopolyether-mediated c... Novel N-Substituted Benzimidazolones as Potent, Selective, CNS-Penetrant, and Orally Active M-1 mAChR Agonists [作者：BUDZIK BRIAN; GARZYA VINCENZO; SHI DONGCHUAN; WALKER GRAHAM; WOOLLEYROBERTS MARIE; PARDOE JOANNE; LUCAS ADAM; TEHAN BEN; RIVERO RALPH A; LANGMEAD CHRISTOPHER J; WATSON JEANNETTE; WU ZINING; FORBES IAN T; JIN JIAN,期刊：ACS Medicinal Chemistry Letters, 页码：244-248 , 文章类型： Article，,卷期：2010年1-6] Virtual screening of the corporate compound collection yielded compound 1 as a subtype selective muscarinic M-1 receptor agonist hit. Initial optimization of the N-capping group of the central piperidine ring resulted in... Development of Fluorescent Ligands for the Human 5-HT1A Receptor [作者：ALONSO DULCE; VAZQUEZVILLA HENAR; GAMO ANA M; MARTINEZESPERON MARIA F; TORTOSA MARIOLA; VISO ALMA; FERNANDEZ DE LA PRADILLA ROBERTO; JUNQUERA ELENA; AICART EMILIO; MARTINFONTECHA MAR; BENHAMU BELLINDA; LOPEZRODRIGUEZ MARIA L; ORTEGAGUTIERREZ SILVIA,期刊：ACS Medicinal Chemistry Letters, 页码：249-253 , 文章类型： Article，,卷期：2010年1-6] In this work, we report the design and synthesis of a set of fluorescent probes targeting the human 5-HT1A receptor (h5-HT1AR). Among the synthesized compounds, derivative 4 deserves special attention as being a high-aff... Carbamylation of N-Terminal Proline [作者：OLAJUYIGBE FOLASADE M; DEMITRI NICOLA; AJELE JOSHUA O; MAURIZIO ELISA; RANDACCIO LUCIO; GEREMIA SILVANO,期刊：ACS Medicinal Chemistry Letters, 页码：254-257 , 文章类型： Article，,卷期：2010年1-6] Protein carbamylation is of great concern both in vivo and in vitro. Here, we report the first structural characterization of a protein carbamylated at the N-terminal proline. The unexpected carbamylation of the a-amino ... Synthesis and Biological Evaluation of Muraymycin Analogues Active against Anti-Drug-Resistant Bacteria [作者：TANINO TETSUYA; ICHIKAWA SATOSHI; ALDABBAGH BAYAN; BOUHSS AHMED; OYAMA HIROSHI; MATSUDA AKIRA,期刊：ACS Medicinal Chemistry Letters, 页码：258-262 , 文章类型： Article，,卷期：2010年1-6] Muraymycin analogues with a lipophilic substituent were synthesized using an Ugi four-component assemblage. This approach provides ready access to a range of analogues simply by altering the aldehyde component. The impac... Quinolizidinone Carboxylic Acids as CNS Penetrant, Selective M-1 Allosteric Muscarinic Receptor Modulators [作者：KUDUK SCOTT D; CHANG RONALD K; DI MARCO CHRISTINA N; RAY WILLIAM J; MA LEI; WITTMANN MARION; SEAGER MATTHEW A; KOEPLINGER KENNETH A; THOMPSON CHARLES D; HARTMAN GEORGE D; BILODEAU MARK T,期刊：ACS Medicinal Chemistry Letters, 页码：263-267 , 文章类型： Article，,卷期：2010年1-6] Positive allosteric modulation of the M, muscarinic receptor represents an approach to treat the cognitive decline in patients with Alzheimer's disease. Replacement of a quinolone ring system in a quinolone carboxylic ac... Identification of a Natural Product Antagonist against the Botulinum Neurotoxin Light Chain Protease [作者：EUBANKS LISA M; SILHAR PETER; SALZAMEDA NICHOLAS T; ZAKHARI JOSEPH S; FENG XIAOCHUAN; BARBIERI JOSEPH T; SHOEMAKER CHARLES B; HIXON MARK S; JANDA KIM D,期刊：ACS Medicinal Chemistry Letters, 页码：268-272 , 文章类型： Article，,卷期：2010年1-6] Botulinum neurotoxins (BoNTs) are the etiological agents responsible for botulism, a disease characterized by peripheral neuromuscular blockade and a characteristic flaccid paralysis of humans. BoNTs are the most lethal ... KSRP/FUBP2 Is a Binding Protein of GO-Y086, a Cytotoxic Curcumin Analogue [作者：YAMAKOSHI HIROYUKI; KANOH NAOKI; KUDO CHIEKO; SATO ATSUKO; UEDA KAZUNORI; MUROI MAKOTO; KON SHUNSUKE; SATAKE MASANOBU; OHORI HISATSUGU; ISHIOKA CHIKASHI; OSHIMA YOSHITERU; OSADA HIROYUKI; CHIBA NATSUKO; SHIBATA HIROYUKI; IWABUCHI YOSHIHARU,期刊：ACS Medicinal Chemistry Letters, 页码：273-276 , 文章类型： Article，,卷期：2010年1-6] Bis(arylmethylidene)acetone derivatives are an important class of curcumin analogues that exhibit various biological and pharmacological activities. We herein report that GO-Y086, a biotinylated bis(arylmethylidene)aceto... Expanded Utility of the beta-Glucuronide Linker: ADCs That Deliver Phenolic Cytotoxic Agents [作者：JEFFREY SCOTT C; DE BRABANDER JEF; MIYAMOTO JAMIE; SENTER PETER D,期刊：ACS Medicinal Chemistry Letters, 页码：277-280 , 文章类型： Article，,卷期：2010年1-6] The beta-glucuronide linker has been used for antibody drug conjugates (ADCs) to deliver amine-containing cytotoxic agents. The linker is stable in circulation, hydrophilic and provides ADCs that are highly active in vit... Understanding Dermatan Sulfate-Heparin Cofactor II Interaction through Virtual Library Screening [作者：RAGHURAMAN ARJUN; MOSIER PHILIP D; DESAI UMESH R,期刊：ACS Medicinal Chemistry Letters, 页码：281-285 , 文章类型： Article，,卷期：2010年1-6] Dermatan sulfate, an important member of the glycosaminoglycan family, interacts with heparin cofactor 11, a member of the serpin family of proteins, to modulate antithrombotic response. Yet, the nature of this interacti... Synthesis and Biochemical Testing of 3-(Carboxyphenylethyl)imidazo[2,1-f][1,2,4]triazines as Inhibitors of AMP Deaminase [作者：LINDELL STEPHEN D; MAECHLING SIMON; SABINA RICHARD L,期刊：ACS Medicinal Chemistry Letters, 页码：286-289 , 文章类型： Article，,卷期：2010年1-6] C-Ribosyl imidazo[2,1-f][1,2,4]triazines and 3-[2-(3-carboxypheny1)ethyl]-3,6,7,8-tetrahydroimidazo[4,5-d][1,3]diaze pin-8-ols represent two classes of known AMP deaminase inhibitors. A combination of the aglycone from t... Discovery of TAK-875: A Potent, Selective, and Orally Bioavailable GPR40 Agonist [作者：NEGORO NOBUYUKI; SASAKI SHINOBU; MIKAMI SATOSHI; ITO MASAHIRO; SUZUKI MASAMI; TSUJIHATA YOSHIYUKI; ITO RYO; HARADA AYAKO; TAKEUCHI KOJI; SUZUKI NOBUHIRO; MIYAZAKI JUNICHI; SANTOU TAKASHI; ODANI TOMOYUKI; KANZAKI NAOYUKI; FUNAMI MIYUKI; TANAKA TOSHIMASA; KOGAME AKIFUMI; MATSUNAGA SHINICHIRO; YASUMA TSUNEO; MOMOSE YU,期刊：ACS Medicinal Chemistry Letters, 页码：290-294 , 文章类型： Article，,卷期：2010年1-6] GPR40, one of the G protein-coupled receptors predominantly expressed in pancreatic beta-cells, mediates enhancement of glucose-stimulated insulin secretion by free fatty acids. A potent and selective GPR40 agonist is th... Labeled Ligand Displacement: Extending NMR-Based Screening of Protein Targets [作者：SWANN STEVEN L; SONG DANYING; SUN CHAOHONG; HAJDUK PHILIP J; PETROS ANDREW M,期刊：ACS Medicinal Chemistry Letters, 页码：295-299 , 文章类型： Article，,卷期：2010年1-6] NMR spectroscopy has enjoyed widespreiad success as a method for screening protein targets, especially in the area of fragment-based drug discovery. However, current methods for NMR-based screening all suffer certain lim...