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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40条记录   Tacrine-Ferulic Acid-Nitric Oxide (NO) Donor Trihybrids as Potent, Multifunctional Acetyl- and Butyrylcholinesterase Inhibitors [作者：CHEN YAO; SUN JIANFEI; FANG LEI; LIU MEI; PENG SIXUN; LIAO HONG; LEHMANN JOCHEN; ZHANG YIHUA,期刊：Journal of Medicinal Chemistry, 页码：4309-4321 , 文章类型： Article，,卷期：2012年55-9] In search of multifunctional cholinesterase inhibitors as potential anti-Alzheimer drug candidates, tacrine-ferulic acid-NO donor trihybrids were synthesized and tested for their cholinesterase inhibitory activities, rel... Discovery and Characterization of an Inhibitor of Glucosylceramide Synthase [作者：RICHARDS STEVEN; LARSON CHRISTOPHER J; KOLTUN ELENA S; HANEL ART; CHAN VICKY; NACHTIGALL JASON; HARRISON AMANDA; AAY NAING; DU HONGWANG; ARCALAS ARLYN; GALAN ADAM; ZHANG JEFF; ZHANG WENTAO; WON KWANGAI; TAM DANNY; QIAN FAWN; WANG TAO; FINN PATRICIA; OGILVIE KATHY; ROSEN JON; AOYAMA RON; PLONOWSKI ARTUR; CANCILLA BELINDA; BENTZIEN FRAUKE; YAKES MICHAEL; MOHAN RAJU; LAMB PETER; NUSS JOHN; KEARNEY PATRICK,期刊：Journal of Medicinal Chemistry, 页码：4322-4335 , 文章类型： Article，,卷期：2012年55-9] Targeting glycosphingolipid synthesis has emerged as a novel approach for treating metabolic diseases. 32 (EXEL-0346) represents a new class of glucosylceramide synthase (GCS) inhibitors. This report details the elaborat... Discovery of New Inhibitors of Cdc25B Dual Specificity Phosphatases by Structure-Based Virtual Screening [作者：LAVECCHIA ANTONIO; DI GIOVANNI CARMEN; PESAPANE ADA; MONTUORI NUNZIA; RAGNO PIA; MARTUCCI NICOLA MASSIMILIANO; MASULLO MARIOROSARIO; DE VENDITTIS EMMANUELE; NOVELLINO ETTORE,期刊：Journal of Medicinal Chemistry, 页码：4142-4158 , 文章类型： Article，,卷期：2012年55-9] Cell division cycle 25 (Cdc25) proteins are highly conserved dual specificity phosphatases that regulate cyclin-dependent kinases and represent attractive drug targets for anticancer therapies. To discover more potent an... De Novo Peptide Design with C3a Receptor Agonist and Antagonist Activities: Theoretical Predictions and Experimental Validation [作者：BELLOWSPETERSON MEGHAN L; FUNG HO KI; FLOUDAS CHRISTODOULOS A,期刊：Journal of Medicinal Chemistry, 页码：4159-4168 , 文章类型： Article，,卷期：2012年55-9] Targeting the complement component 3a receptor (C3aR) with selective agonists or antagonists is believed to be a viable therapeutic option for several diseases such as stroke, heart attack, reperfusion injuries, and rheu... Novel 1,2,4-Triazolo[1,5-a]pyridines and Their Fused Ring Systems Attenuate Oxidative Stress and Prolong Lifespan of Caenorhabiditis elegans [作者：MEKHEIMER RAMADAN AHMED; SAYED AHMED AMIR RADWAN; AHMED ELTAIB ALI,期刊：Journal of Medicinal Chemistry, 页码：4169-4177 , 文章类型： Article，,卷期：2012年55-9] In this paper we report the synthesis of some novel 1,2,4-triazolo [1,5-a]pyridine and azolotriazolopyridine ring systems. The products were screened for various types of activity like antibacterial, antifungal, and anti... A New Promising Application for Highly Cytotoxic Metal Compounds: eta(6)-Areneruthenium(II) Phosphite Complexes for the Treatment of Alveolar Echinococcosis [作者：KUESTER TATIANA; LENSE NADINE; BARNA FABIENNE; HEMPHILL ANDREW; KINDERMANN MARKUS K; HEINICKE JOACHIM W; VOCK CARSTEN A,期刊：Journal of Medicinal Chemistry, 页码：4178-4188 , 文章类型： Article，,卷期：2012年55-9] Two series of eta(6)-areneruthenium(II) phosphite complexes were prepared, characterized, and evaluated in vitro for their toxic potential against Echinococcus multilocularis metacestodes. Neutral complexes of general fo... Analogues of Fenarimol Are Potent Inhibitors of Trypanosoma cruzi and Are Efficacious in a Murine Model of Chagas Disease [作者：KEENAN MARTINE; ABBOTT MICHAEL J; ALEXANDER PAUL W; ARMSTRONG TANYA; BEST WAYNE M; BERVEN BRADLEY; BOTERO ADRIANA; CHAPLIN JASON H; CHARMAN SUSAN A; CHATELAIN ERIC; VON GELDERN THOMAS W; KERFOOT MARIA; KHONG ANDREA; TIEN NGUYEN; MCMANUS JOSHUA D; MORIZZI JULIA; RYAN EILEEN; SCANDALE IVAN; THOMPSON R ANDREW; WANG SEN Z; WHITE KAREN L,期刊：Journal of Medicinal Chemistry, 页码：4189-4204 , 文章类型： Article，,卷期：2012年55-9] We report the discovery of nontoxic fungicide fenarimol (1) as an inhibitor of Trypanosoma cruzi (T. cruzi), the causative agent of Chagas disease, and the results of structure-activity investigations leading to potent a... Synthesis, Structure-Activity Relationship, and Pharmacological Studies of Novel Melanin-Concentrating Hormone Receptor 1 Antagonists 3-Aminomethylquinolines: Reducing Human Ether-a-go-go-Related Gene (hERG) Associated Liabilities [作者：KASAI SHIZUO; KAMATA MAKOTO; MASADA SHINICHI; KUNITOMO JUN; KAMAURA MASAHIRO; OKAWA TOMOHIRO; TAKAMI KAZUAKI; OGINO HITOMI; NAKANO YOSHIHIDE; ASHINA SHUNTAROU; WATANABE KAORU; KAISHO TOMOKO; IMAI YUMI N; RYU SUNGHI; NAKAYAMA MASAHARU; NAGISA YASUTAKA; TAKEKAWA SHIRO; KATO KOKI; MURATA TOSHIKI; SUZUKI NOBUHIRO; ISHIHARA YUJI,期刊：Journal of Medicinal Chemistry, 页码：4336-4351 , 文章类型： Article，,卷期：2012年55-9] Recently, we discovered 3-aminomethylquinoline derivative 1, a selective, highly potent, centrally acting, and orally bioavailable human MCH receptor 1 (hMCHR1) antagonist, that inhibited food intake in F344 rats with di... A 20S Combined with a 22R Configuration Markedly Increases both in Vivo and in Vitro Biological Activity of 1 alpha,25-Dihydroxy-22-methyl-2-methylene-19-norvitamin D-3 [作者：FLORES AGNIESZKA; SICINSKI RAFAL R; GRZYWACZ PAWEL; THODEN JAMES B; PLUM LORI A; CLAGETTDAME MARGARET; DELUCA HECTOR F,期刊：Journal of Medicinal Chemistry, 页码：4352-4366 , 文章类型： Article，,卷期：2012年55-9] Six new analogues of 1 alpha,25-dihydroxy-19-norvitamin D-3 (3a-4b, 5, and 6) were prepared by a convergent synthesis applying the Wittig-Horner reaction as a key step. The influence of methyl groups at C-22 on their bio... Head-to-Head Prenyl Tranferases: Anti-Infective Drug Targets [作者：LIN FUYANG; LIU YILIANG; LI KAI; CAO RONG; ZHU WEI; AXELSON JORDAN; PANG RAN; OLDFIELD ERIC,期刊：Journal of Medicinal Chemistry, 页码：4367-4372 , 文章类型： Article，,卷期：2012年55-9] We report X-ray crystallographic structures of three inhibitors bound to dehydrosqualene synthase from Staphylococcus aureus: 1 (BPH-651), 2 (WC-9), and 3 (SQ-109). Compound 2 binds to the S2 site with its -SCN group sur... Butyl Pocket Formation in the Vitamin D Receptor Strongly Affects the Agonistic or Antagonistic Behavior of Ligands [作者：YOSHIMOTO NOBUKO; SAKAMAKI YUTA; HAETA MINORU; KATO AKIRA; INABA YUKA; ITOH TOSHIMASA; NAKABAYASHI MAKOTO; ITO NOBUTOSHI; YAMAMOTO KEIKO,期刊：Journal of Medicinal Chemistry, 页码：4373-4381 , 文章类型： Article，,卷期：2012年55-9] Previously, we reported that 22S-butyl-25,26,27-trinor-1 alpha,24-dihydroxyvitamin D-3 2 represents a new class of antagonist for the vitamin D receptor (VDR). The crystal structure of the ligand-binding domain (LBD) of ... Synthesis and Biological Evaluation of 4-Phenylquinazoline-2-carboxamides Designed as a Novel Class of Potent Ligands of the Translocator Protein [作者：CASTELLANO SABRINA; TALIANI SABRINA; MILITE CIRO; PUGLIESI ISABELLA; DA POZZO ELEONORA; RIZZETTO ELISA; BENDINELLI SARA; COSTA BARBARA; COSCONATI SANDRO; GRECO GIOVANNI; NOVELLINO ETTORE; SBARDELLA GIANLUCA; STEFANCICH GIORGIO; MARTINI CLAUDIA; DA SETTIMO FEDERICO,期刊：Journal of Medicinal Chemistry, 页码：4506-4510 , 文章类型： Article，,卷期：2012年55-9] A series of novel 4-phenylquinazoline-2-carboxamides (1-58) were designed as aza-isosters of PK11195, the wellknown 18 kDa translocator protein (TSPO) reference ligand, and synthesized by means of a very simple and effic... Discovery of a Potent and Selective GPR120 Agonist [作者：SHIMPUKADE BHARAT; HUDSON BRIAN D; HOVGAARD CHRISTINE KIEL; MILLIGAN GRAEME; ULVEN TROND,期刊：Journal of Medicinal Chemistry, 页码：4511-4515 , 文章类型： Article，,卷期：2012年55-9] GPR120 is a receptor of unsaturated long-chain fatty acids reported to mediate GLP-1 secretion, insulin sensitization, anti-inflammatory, and anti-obesity effects and is therefore emerging as a new potential target for t... Synthesis and Antitumor Efficacy of a beta-Glucuronidase-Responsive Albumin-Binding Prodrug of Doxorubicin [作者：LEGIGAN THIBAUT; CLARHAUT JONATHAN; RENOUX BRIGITTE; TRANOYOPALINSKI ISABELLE; MONVOISIN ARNAUD; BERJEAUD JEANMARC; GUILHOT FRANCOIS; PAPOT SEBASTIEN,期刊：Journal of Medicinal Chemistry, 页码：4516-4520 , 文章类型： Article，,卷期：2012年55-9] In this paper we describe the synthesis and biological evaluation of the first beta-glucuronidase-responsive albumin-binding prodrug designed for the selective delivery of doxorubicin at the tumor site. This prodrug lead... Fluorocyclopentenyl-cytosine with Broad Spectrum and Potent Antitumor Activity [作者：CHOI WON JUN; CHUNG HWAJIN; CHANDRA GIRISH; ALEXANDER VARUGHESE; ZHAO LONG XUAN; LEE HYUK WOO; NAYAK AKSHATA; MAJIK MAHESH S; KIM HEA OK; KIM JINHEE; LEE YOUNG B; AHN CHANG H; LEE SANG KOOK; JEONG LAK SHIN,期刊：Journal of Medicinal Chemistry, 页码：4521-4525 , 文章类型： Article，,卷期：2012年55-9] On the basis of the potent biological activity of cyclopentenyl-pyrimidines, fluorocyclopentenyl-pyrimidines were designed and synthesized from D-ribose. Among these, the cytosine derivative 5a showed highly potent antig... Synthesis, Structure-Affinity Relationships, and Radiolabeling of Selective High-Affinity 5-HT4 Receptor Ligands as Prospective Imaging Probes for Positron Emission Tomography (vol 53, pg 7035, 2010) [作者：XU RONG; HONG JINSOO; MORSE CHERYL L; PIKE VICTOR W,期刊：Journal of Medicinal Chemistry, 页码：4526-4526 , 文章类型： Correction，,卷期：2012年55-9]