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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   Inhibitors of Prolyl Oligopeptidases for the Therapy of Human Diseases: Defining Diseases and Inhibitors [作者：LAWANDI JANICE; GERBERLEMAIRE SANDRINE; JUILLERATJEANNERET LUCIENNE; MOITESSIER NICOLAS,期刊：Journal of Medicinal Chemistry, 页码：3423-3438 , 文章类型： Article，,卷期：2010年53-9] Small Molecules and Stem Cells. Potency and Lineage Commitment: The New Quest for the Fountain of Youth [作者：LUKASZEWICZ AGNES I; MCMILLAN MICHAEL K; KAHN MICHAEL,期刊：Journal of Medicinal Chemistry, 页码：3439-3453 , 文章类型： Article，,卷期：2010年53-9] Synthesis, Chiral High Performance Liquid Chromatographic Resolution and Enantiospecific Activity of a Potent New Geranylgeranyl Transferase Inhibitor, 2-Hydroxy-3-imidazo[1,2-a]pyridin-3-yl-2-phosphonopropionic Acid [作者：MCKENNA CHARLES E; KASHEMIROV BORIS A; BLAZEWSKA KATARZYNA M; MALLARDFAVIER ISABELLE; STEWART CHARLOTTE A; ROJAS JAVIER; LUNDY MARK W; EBETINO FRANK H; BARON RUDI A; DUNFORD JAMES E; KIRSTEN MARIE L; SEABRA MIGUEL C; BALA JOY L; MARMA MONG S; ROGERS MICHAEL J; COXON FRASER P,期刊：Journal of Medicinal Chemistry, 页码：3454-3464 , 文章类型： Article，,卷期：2010年53-9] 3-(3-Pyridyl)-2-hydroxy-2-phosphonopropanoic acid (3-PEHPC, 1) is a phosphonocarboxylate (PC) analogue of 2-(3-pyridyl)-1-hydroxyethylidenebis(phosphonic acid) (risedronic acid, 2), an osteoporosis drug that decreases bo... Design, Synthesis, and Interaction Study of Quinazoline-2(1H)-thione Derivatives as Novel Potential Bcl-x(L) Inhibitors [作者：FENG YU; DING XIAO; CHEN TAO; CHEN LILI; LIU FANG; JIA XU; LUO XIAOMIN; SHEN XU; CHEN KAIXIAN; JIANG HUALIANG; WANG HUI; LIU HONG; LIU DONGXIANG,期刊：Journal of Medicinal Chemistry, 页码：3465-3479 , 文章类型： Article，,卷期：2010年53-9] Development of inhibitors to antagonize the activities of antiapoptotic Bcl-2 family proteins is of particular interest in cancer chemotherapy. We discovered a quinazoline-2(1H)-thione derivative (DCBL55) as a new Bcl-x(... "Viologen" Dendrimers as Antiviral Agents: The Effect of Charge Number and Distance [作者：ASAFTEI SIMONA; DE CLERCQ ERIK,期刊：Journal of Medicinal Chemistry, 页码：3480-3488 , 文章类型： Article，,卷期：2010年53-9] A series of "viologen" derivatives (4,4'-bipyridinium salts) carrying between 1 and 90 charges per molecule have been prepared and investigated for their activity against human immunodeficiency virus (HIV), herpes simple... Frontal Affinity Chromatography-Mass Spectrometry Useful for Characterization of New Ligands for GPR17 Receptor [作者：CALLERI ENRICA; CERUTI STEFANIA; CRISTALLI GLORIA; MARTINI CLAUDIA; TEMPORINI CATERINA; PARRAVICINI CHIARA; VOLPINI ROSARIA; DANIELE SIMONA; CACCIALANZA GABRIELE; LECCA DAVIDE; LAMBERTUCCI CATIA; TRINCAVELLI MARIA LETIZIA; MARUCCI GABRIELLA; WAINER IRVING W; RANGHINO GRAZIELLA; FANTUCCI PIERCARLO; ABBRACCHIO MARIA P; MASSOLINI GABRIELLA,期刊：Journal of Medicinal Chemistry, 页码：3489-3501 , 文章类型： Article，,卷期：2010年53-9] The application of frontal affinity chromatography mass spectrometry (FAC-MS), along with molecular modeling studies, to the screening of potential drug candidates toward the recently deorphanized G-protein-coupled recep... Discovery of Novel and Potent Leukotriene B-4 Receptor Antagonists. Part 1 [作者：GOODNOW ROBERT A JR; HICKS ALEXANDRA; SIDDURI ACHYUTHARAO; KOWALCZYK AGNIESZKA; DOMINIQUE ROMYR; QIAO QI; LOU JIAN PING; GILLESPIE PAUL; FOTOUHI NADER; TILLEY JEFFERSON; COHEN NOAL; CHOUDHRY SATISH; CAVALLO GARY; TANNU SHAHID A; VENTRE JESSICA D; LAVELLE DANIELLE; TARE NADINE S; OH HYESUN; LAMB MARTIN; KURYLKO GRAZYNA; HAMID RACHID; WRIGHT MATTHEW B; PAMIDIMUKKALA ANJULA; EGAN THOMAS; GUBLER UELI; HOFFMAN ANN F; WEI XIN; LI YING L; ONEIL JOHN; MARCANO RUBEN; POZZANI KAREN; MOLINARO TINA; SANTIAGO JENNIFER; SINGER LAURA; HARGADEN MAUREEN; MOORE DAVID; CATALA A ROBERT; CHAO LISA C F; HERMANN GESINE; VENKAT RADHIKA; MANCEBO HELENA; RENZETTI LOUIS M,期刊：Journal of Medicinal Chemistry, 页码：3502-3516 , 文章类型： Article，,卷期：2010年53-9] The inhibition of LTB4 binding to and activation of G-protein-coupled receptors BLT1 and BLT2 is the premise of a treatment for several inflammatory diseases. In a lead optimization effort starting with the leukotriene B... Discovery of a Tetrahydropyrimidin-2(1H)-one Derivative (TAK-442) as a Potent, Selective, and Orally Active Factor Xa Inhibitor [作者：FUJIMOTO TAKUYA; IMAEDA YASUHIRO; KONISHI NORIKO; HIROE KATSUHIKO; KAWAMURA MASAKI; TEXTOR GARRET P; AERTGEERTS KATHLEEN; KUBO KEIJI,期刊：Journal of Medicinal Chemistry, 页码：3517-3531 , 文章类型： Article，,卷期：2010年53-9] Coagulation enzyme factor Xa (FXa) is a particularly promising target for the development of new anticoagulant agents. We previously reported the imidazo[1,5-c]imidazol-3-one derivative 1 as a potent and orally active FX... Identification of 4,5-Dihydro-1H-pyrazolo[4,3-h]quinazoline Derivatives as a New Class of Orally and Selective Polo-Like Kinase 1 Inhibitors [作者：BERIA ITALO; BALLINARI DARIO; BERTRAND JAY AARON; BORGHI DANIELA; BOSSI ROBERTO TIBERIO; BRASCA MARIA GABRIELLA; CAPPELLA PAOLO; CARUSO MICHELE; CECCARELLI WALTER; CIAVOLELLA ANTONELLA; CRISTIANI CINZIA; CROCI VALTER; DE PONTI ANNA; FACHIN GABRIELE; FERGUSON RONALD DALE; LANSEN JACQUELINE; MOLL JURGEN KARL; PESENTI ENRICO; POSTERI HELENA; PEREGO RITA; ROCCHETTI MAURIZIO; STORICI PAOLA; VOLPI DANIELE; VALSASINA BARBARA,期刊：Journal of Medicinal Chemistry, 页码：3532-3551 , 文章类型： Article，,卷期：2010年53-9] Polo-like kinase 1 (Plk1) is a fundamental regulator of mitotic progression whose overexpression is often associated with oncogenesis and therefore is recognized as an attractive therapeutic target in the treatment of pr... A Repurposing Strategy Identifies Novel Synergistic Inhibitors of Plasmodium falciparum Heat Shock Protein 90 [作者：SHAHINAS DEA; LIANG MICHAEL; DATTI ALESSANDRO; PILLAI DYLAN R,期刊：Journal of Medicinal Chemistry, 页码：3552-3557 , 文章类型： Article，,卷期：2010年53-9] Malaria is responsible for 3 million deaths annually. Antimalarial drug resistance is widespread, and few novel, well-defined targets exist. A robotic high throughput screen (HTS) was performed using 4000 small molecules... Antimicrobial Activity of Tryptanthrins in Escherichia coli [作者：BANDEKAR POOJA P; ROOPNARINE KEIR ALEKSEII; PAREKH VIRALI J; MITCHELL THOMAS R; NOVAK MARK J; SINDEN RICHARD R,期刊：Journal of Medicinal Chemistry, 页码：3558-3565 , 文章类型： Article，,卷期：2010年53-9] Tryptanthrins have potential therapeutic activity against a wide variety of pathogenic organisms, although little is known about their mechanism. Activity against Escherichia colt, however, has not been examined. The eff... How Well Can the Caco-2/Madin-Darby Canine Kidney Models Predict Effective Human Jejunal Permeability? [作者：AVDEEF ALEX; TAM KIN Y,期刊：Journal of Medicinal Chemistry, 页码：3566-3584 , 文章类型： Article，,卷期：2010年53-9] The study aimed to predict effective human jejunal permeability (P-eff) using a biophysical model based on parametrized paracellular, aqueous boundary layer, and transcellular permeabilities, and the villus-fold surface ... Investigation of the Bioactive Conformation of Histamine H-3 Receptor Antagonists by the Cyclopropylic Strain-Based Conformational Restriction Strategy [作者：WATANABE MIZUKI; HIROKAWA TAKATSUGU; KOBAYASHI TAKAAKI; YOSHIDA AKIRA; ITO YOSHIHIKO; YAMADA SHIZUO; ORIMOTO NAOKI; YAMASAKI YASUNDO; ARISAWA MITSUHIRO; SHUTO SATOSHI,期刊：Journal of Medicinal Chemistry, 页码：3585-3593 , 文章类型： Article，,卷期：2010年53-9] We previously identified the highly potent histamine H-3 receptor antagonists (1R,2S)-2-[2-(4-chlorobenzylamino)ethyl]-1-(1H-imidazol-4-yl)cyclopropa ne (1) and its enantiomer ent-1. Although the conformations of 1 and e... Thiazole, Oxadiazole, and Carboxamide Derivatives of Artemisinin are Highly Selective and Potent Inhibitors of Toxoplasma gondii [作者：HENCKEN CHRISTOPHER P; JONESBRANDO LORRAINE; BORDON CLAUDIA; STOHLER REMO; MOTT BRYAN T; YOLKEN ROBERT; POSNER GARY H; WOODARD LAUREN E,期刊：Journal of Medicinal Chemistry, 页码：3594-3601 , 文章类型： Article，,卷期：2010年53-9] We have prepared 23 new dehydroartemisinin (DART) trioxane derivatives (11 thiazoles, 2 oxadiazoles, and 10 carboxamides) and have screened them for in vitro activity in the Toxoplasma lytic cycle. Fifteen (65%) of the d... Potent and Selective Fluoroketone Inhibitors of Group VIA Calcium-Independent Phospholipase A(2) [作者：KOKOTOS GEORGE; HSU YUANHAO; BURKE JOHN E; BASKAKIS CONSTANTINOS; KOKOTOS CHRISTOFOROS G; MAGRIOTI VICTORIA; DENNIS EDWARD A,期刊：Journal of Medicinal Chemistry, 页码：3602-3610 , 文章类型： Article，,卷期：2010年53-9] Group VIA calcium-independent phospholipase A(2) (GVIA 1PLA(2)) has recently emerged as a novel pharmaceutical target. We have now explored the structure activity relationship between fluoroketones and GVIA iPLA(2) inhib... Bivalent beta-Carbolines as Potential Multitarget Anti-Alzheimer Agents [作者：ROOK YVONNE; SCHMIDTKE KAIUWE; GAUBE FRIEDEMANN; SCHEPMANN DIRK; WUENSCH BERNHARD; HEILMANN JOERG; LEHMANN JOCHEN; WINCKLER THOMAS,期刊：Journal of Medicinal Chemistry, 页码：3611-3617 , 文章类型： Article，,卷期：2010年53-9] Alzheimer's disease (AD) is a prevalent neurodegenerative disorder with multifactorial causes that requires multitargeted treatment. Inhibitors of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) improve chol...