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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32条记录   Sulfonylureas Have Antifungal Activity and Are Potent Inhibitors of Candida albicans Acetohydroxyacid Synthase [作者：LEE YUTING; CUI CHANGJUN; CHOW EVE W L; PUE NASON; LONHIENNE THIERRY; WANG JIANGUO; FRASER JAMES A; GUDDAT LUKE W,期刊：Journal of Medicinal Chemistry, 页码：210-219 , 文章类型： Article，,卷期：2013年56-1] The sulfonylurea herbicides exert their activity by inhibiting plant acetohydroxyacid synthase (AHAS), the first enzyme in the branched-chain amino acid biosynthesis pathway. It has previously been shown that if the gene... Discovery of Agonists of Cannabinoid Receptor 1 with Restricted Central Nervous System Penetration Aimed for Treatment of Gastroesophageal Reflux Disease [作者：PLOWRIGHT ALLEYN T; NILSSON KAROLINA; ANTONSSON MADELEINE; AMIN KOSRAT; BRODDEFALK JOHAN; JENSEN JORGEN; LEHMANN ANDERS; JIN SHUJUAN; STONGE STEPHANE; TOMASZEWSKI MIROSLAW J; TREMBLAY MAXIME; WALPOLE CHRISTOPHER; WEI ZHONGYONG; YANG HUA; ULANDER JOHAN,期刊：Journal of Medicinal Chemistry, 页码：220-240 , 文章类型： Article，,卷期：2013年56-1] Agonists of the cannabinoid receptor 1 (CB1) have been suggested as possible treatments for a range of medical disorders including gastroesophageal reflux disease (GERD). While centrally acting cannabinoid agonists are k... Dibenzosuberones as p38 Mitogen-Activated Protein Kinase Inhibitors with Low ATP Competitiveness and Outstanding Whole Blood Activity [作者：FISCHER STEFAN; WENTSCH HEIKE K; MAYERWRANGOWSKI SVENJA C; ZIMMERMANN MARKUS; BAUER SILKE M; STORCH KIRSTEN; NIESS RAIMUND; KOEBERLE SOLVEIGH C; GRUETTER CHRISTIAN; BOECKLER FRANK M; RAUH DANIEL; LAUFER STEFAN A,期刊：Journal of Medicinal Chemistry, 页码：241-253 , 文章类型： Article，,卷期：2013年56-1] p38 alpha mitogen-activated protein (MAP) kinase is a main target in drug research concerning inflammatory diseases. Nevertheless, no inhibitor of p38 alpha MAP kinase has been introduced to the market. This might be att... An Optimized RAD51 Inhibitor That Disrupts Homologous Recombination without Requiring Michael Acceptor Reactivity [作者：BUDKE BRIAN; KALIN JAY H; PAWLOWSKI MICHAL; ZELIVIANSKAIA ANNA S; WU MEGAN; KOZIKOWSKI ALAN P; CONNELL PHILIP P,期刊：Journal of Medicinal Chemistry, 页码：254-263 , 文章类型： Article，,卷期：2013年56-1] Homologous recombination (HR) is an essential process in cells that provides repair of DNA double-strand breaks and lesions that block DNA replication. RAD51 is an evolutionarily conserved protein that is central to HR. ... 3,6-Diamino-4-(2-halophenyl)-2-benzoylthieno[2,3-b]pyridine-5-carbonitri les Are Selective Inhibitors of Plasmodium falciparum Glycogen Synthase Kinase-3 [作者：FUGEL WIEBKE; OBERHOLZER ANSELM ERICH; GSCHLOESSL BERNHARD; DZIKOWSKI RON; PRESSBURGER NARKISS; PREU LUTZ; PEARL LAURENCE H; BARATTE BLANDINE; RATIN MORGANE; OKUN ILYA; DOERIG CHRISTIAN; KRUGGEL SEBASTIAN; LEMCKE THOMAS; MEIJER LAURENT; KUNICK CONRAD,期刊：Journal of Medicinal Chemistry, 页码：264-275 , 文章类型： Article，,卷期：2013年56-1] Plasmodium falciparum is the infective agent responsible for malaria tropica. The glycogen synthase kinase-3 of the parasite (Pf GSK-3) was suggested as a potential biological target for novel antimalarial drugs. Startin... Garcinia Xanthones as Orally Active Antitumor Agents [作者：ZHAN XIAOJIN; LI XIANG; SUN HAOPENG; WANG XIAOJIAN; ZHAO LI; GAO YUAN; LIU XIAORONG; ZHANG SHENGLIE; WANG YANYAN; YANG YINGRUI; ZENG SU; GUO QINGLONG; YOU QIDONG,期刊：Journal of Medicinal Chemistry, 页码：276-292 , 文章类型： Article，,卷期：2013年56-1] Using a newly developed strategy whose key step is the regioselective propargylation of hydroxyxanthone substrates, 99 structurally diverse Garcinia natural-product-like xanthones based on gambogic acid were designed and... Sulfocounnarins (1,2-Benzoxathiine-2,2-dioxides): A Class of Potent and Isoform-Selective Inhibitors of Tumor-Associated Carbonic Anhydrases [作者：TARS KASPARS; VULLO DANIELA; KAZAKS ANDRIS; LEITANS JANIS; LENDS ALONS; GRANDANE AIGA; ZALUBOVSKIS RAIVIS; SCOZZAFAVA ANDREA; SUPURAN CLAUDIU T,期刊：Journal of Medicinal Chemistry, 页码：293-300 , 文章类型： Article，,卷期：2013年56-1] Coumarins were recently shown to constitute a novel class of mechanism-based carbonic anhydrase (CA, EC 4.2.1.1) inhibitors. We demonstrate that sulfocoumarins (1,2-benzoxathiine 2,2-dioxides) possess a similar mechanism... Design and Synthesis of Diazatricyclodecane Agonists of the G-Protein-Coupled Receptor 119 [作者：DAROUT ETZER; ROBINSON RALPH P; MCCLURE KIM F; CORBETT MATTHEW; LI BRYAN; SHAVNYA ANDREI; ANDREWS MELISSA P; JONES CHRISTOPHER S; LI QIFANG; MINICH MARTHA L; MASCITTI VINCENT; GUIMARAES CRISTIANO R W; MUNCHHOF MICHAEL J; BAHNCK KEVIN B; CAI CUIMAN; PRICE DAVID A; LIRAS SPIROS; BONIN PAUL D; CORNELIUS PETER; WANG RUDUAN; BAGDASARIAN VICTORIA; SOBOTA COLLEEN P; HORNBY SAM; MASTERSON VICTORIA M; JOSEPH REENA M; KALGUTKAR AMIT S; CHEN YUE,期刊：Journal of Medicinal Chemistry, 页码：301-319 , 文章类型： Article，,卷期：2013年56-1] A series of GPR119 agonists based on a 2,6-diazatricyclo[3.3.1.1 similar to 3,7,similar to]decane ring system is described. Also provided is a detailed account of the development of a multigram scale synthesis of the dia... Synthesis and Insight into the Structure-Activity Relationships of Chalcones as Antimalarial Agents [作者：TADIGOPPULA NARENDER; KORTHIKUNTA VENKATESWARLU; GUPTA SHWETA; KANCHARLA PAPIREDDY; KHALIQ TANVIR; SONI AWAKASH; SRIVASTAVA RAJEEV KUMAR; SRIVASTAVA KUMKUM; PURI SUNIL KUMAR; RAJU KANUMURI SIVA RAMA; WAHAJUDDIN; SIJWALI PURAN SINGH; KUMAR VIKASH; MOHAMMAD IMRAN SIDDIQI,期刊：Journal of Medicinal Chemistry, 页码：31-45 , 文章类型： Article，,卷期：2013年56-1] Licochalcone A (I), isolated from the roots of Chinese licorice, is the most promising antimalarial compound reported so far. In continuation of our drug discovery program, we isolated two similar chalcones, medicagenin ... Peptide-Conjugated Pterins as Inhibitors of Ricin Toxin A [作者：SAITO RYOTA; PRUET JEFF M; MANZANO LAWRENCE A; JASHEWAY KARL; MONZINGO ARTHUR F; WIGET PAUL A; KAMAT ISHAN; ANSLYN ERIC V; ROBERTUS JON D,期刊：Journal of Medicinal Chemistry, 页码：320-329 , 文章类型： Article，,卷期：2013年56-1] Several 7-peptide-substituted pterins were synthesized and tested as competitive active-site inhibitors of ricin toxin A (RTA). Focus began on dipeptide conjugates, and these results further guided the construction of se... Theoretical Investigations and Density Functional Theory Based Quantitative Structure-Activity Relationships Model for Novel Cytotoxic Platinum(IV) Complexes [作者：VARBANOV HRISTO P; JAKUPEC MICHAEL A; ROLLER ALEXANDER; JENSEN FRANK; GALANSKI MARKUS; KEPPLER BERNHARD K,期刊：Journal of Medicinal Chemistry, 页码：330-344 , 文章类型： Article，,卷期：2013年56-1] Octahedral platinum(IV) complexes are promising candidates in the fight against cancer. In order to rationalize the further development of this class of compounds, detailed studies on their mechanisms of action, toxicity... 3-Amido Pyrrolopyrazine JAK Kinase Inhibitors: Development of a JAK3 vs JAK1 Selective Inhibitor and Evaluation in Cellular and in Vivo Models [作者：SOTH MICHAEL; HERMANN JOHANNES C; YEE CALVIN; ALAM MUZAFFAR; BARNETT JIM W; BERRY PAMELA; BROWNER MICHELLE F; FRANK KARL; FRAUCHIGER SANDRA; HARRIS SETH; HE YANG; HEKMATNEJAD MOHAMMAD; HENDRICKS THAN; HENNINGSEN ROBERT; HILGENKAMP RAMONA; HO HOANGDUNG; HOFFMAN ANN; HSU PEIYUAN; HU DONGQING; ITANO ANDREA; JAIMEFIGUEROA SAUL; JAHANGIR ALAM; JIN SUE; KUGLSTATTER ANDREAS; KUTACH ALAN K; LIAO CHENG; LYNCH STEPHEN; MENKE JOHN; NIU LINGHAO; PATEL VAISHALI; RAILKAR ARUNA; ROY DOUGLAS; SHAO ADA; SHAW DAVID; STEINER SANDRA; SUN YONGLIANG; TAN SENGLAI; WANG SANDRA; MINH DIEM VU,期刊：Journal of Medicinal Chemistry, 页码：345-356 , 文章类型： Article，,卷期：2013年56-1] The Janus kinases (JAKs) are involved in multiple signaling networks relevant to inflammatory diseases, and inhibition of one or more members of this class may modulate disease activity or progression. We optimized a new... Alkyl Substituted 2 '-Benzoylpyridine Thiosemicarbazone Chelators with Potent and Selective Anti-Neoplastic Activity: Novel Ligands that Limit Methemoglobin Formation [作者：STEFANI CHRISTIAN; JANSSON PATRIC J; GUTIERREZ ELAINE; BERNHARDT PAUL V; RICHARDSON DES R; KALINOWSKI DANUTA S,期刊：Journal of Medicinal Chemistry, 页码：357-370 , 文章类型： Article，,卷期：2013年56-1] Thiosemicarbazone chelators, including the 2'-benzoylpyridine thiosemicarbazones (BpT) class, show marked potential as anticancer agents. Importantly, 3-aminopyridine-2-carboxaldehyde thiosemicarbazone (3-AP) has been in... Discovery of Novel and Ligand-Efficient Inhibitors of Plasmodium falciparum and Plasmodium vivax N-Myristoyltransferase [作者：RACKHAM MARK D; BRANNIGAN JAMES A; MOSS DAVID K; YU ZHIYONG; WILKINSON ANTHONY J; HOLDER ANTHONY A; TATE EDWARD W; LEATHERBARROW ROBIN J,期刊：Journal of Medicinal Chemistry, 页码：371-375 , 文章类型： Article，,卷期：2013年56-1] N-Myristoyltransferase (NMT) is an attractive antiprotozoan drug target. A lead-hopping approach was utilized in the design and synthesis of novel benzo[b]thiophene-containing inhibitors of Plasmodium falciparum (PO and ... Alpha-Heteroatorn Derivatized Analogues of 3-(Acetylhydroxyamino)propyl Phosphonic Acid (FR900098) as Antimalarials [作者：VERBRUGGHEN THOMAS; VANDURM PIERRE; POUYEZ JENNY; MAES LOUIS; WOUTERS JOHAN; VAN CALENBERGH SERGE,期刊：Journal of Medicinal Chemistry, 页码：376-380 , 文章类型： Article，,卷期：2013年56-1] To explore the hitherto successful derivatization of the alpha-carbon of fosmidomycin, a series of new a-substituted analogues was prepared. This was done by introduction of a heteroatom (N or O) in alpha-position to the... Development of Vizantin, a Safe Immunostimulant, Based on the Structure-Activity Relationship of Trehalose-6,6 '-dicorynomycolate [作者：YAMAMOTO HIROFUMI; ODA MASATAKA; NAKANO MAYO; WATANABE NAOYUKI; YABIKU KENTA; SHIBUTANI MASAHIRO; INOUE MASAHISA; IMAGAWA HIROSHI; NAGAHAMA MASAHIRO; HIMENO SEIICHIRO; SETSU KOJUN; SAKURAI JUN; NISHIZAWA MUGIO,期刊：Journal of Medicinal Chemistry, 页码：381-385 , 文章类型： Article，,卷期：2013年56-1] Vizantin, 6,6'-bis-O-(3-nonyldodecanoy1)-alpha,alpha'-trehalose, was developed as a safe immunostimulator on the basis of a structure-activity relationship (SAR) study with trehalose 6,6'-dicorynomycolate (TDCM). It was ...