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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57条记录   Pyrrolidine Analogues of Lobelane: Relationship of Affinity for the Dihydrotetrabenazine Binding Site with Function of the Vesicular Monoamine Transporter 2 (VMAT2) [作者：VARTAK ASHISH P; NICKEL JUSTIN R; CHAGKUTIP JATURAPORN; DWOSKIN LINDA P; CROOKS PETER A,期刊：Journal of Medicinal Chemistry, 页码：7878-7882 , 文章类型： Article，,卷期：2009年52-23] Ring size reduction of the central piperidine ring of lobelane yielded pyrrolidine analogues that showed marked inconsistencies in their ability to bind to the dihydrotetrabenazine (DTBZ) binding site on the vesicular mo... Toward a Rational Design of Multitarget-Directed Antioxidants: Merging Memoquin and Lipoic Acid Molecular Frameworks [作者：BOLOGNESI MARIA LAURA; CAVALLI ANDREA; BERGARMINI CHRISTIAN; FATO ROMANA; LENAZ GIORGIO; ROSINI MICHELA; BARTOLINI MANUELA; ANDRISANO VINCENZA; MELCHIORRE CARLO,期刊：Journal of Medicinal Chemistry, 页码：7883-7886 , 文章类型： Article，,卷期：2009年52-23] Novel multitargeted antioxidants 3-6 were designed by combining the antioxidant features, namely, a benzoquinone fragment and a lipoyl function, of two multifunctional lead candidates. They were then evaluated to determi... Betulinic Acid Derivatives as Human Immunodeficiency Virus Type 2 (HIV-2) Inhibitors [作者：DANG ZHAO; LAI WEIHONG; QIAN KEDUO; HO PHONG; LEE KUOHSIUNG; CHEN CHINHO; HUANG LI,期刊：Journal of Medicinal Chemistry, 页码：7887-7891 , 文章类型： Article，,卷期：2009年52-23] We previously reported that [[N-[3 beta-hydroxyllup-20(29)-en-28-oyl]-7-aminoheptyl]carbamoyl]methane (A43D, 4) was a potent HIV-1 entry inhibitor. However, 4 was inactive against HIV-2 virus, suggesting the structural r... Synthesis and Characterization of Environment-Sensitive Fluorescent Ligands for Human 5-HT1A Receptors with 1-Arylpiperazine Structure [作者：LACIVITA ENZA; LEOPOLDO MARCELLO; MASOTTI ANNA CARMELA; INGLESE CARMELA; BERARDI FRANCESCO; PERRONE ROBERTO; GANGULY SOURAV; JAFURULLA MD; CHATTOPADHYAY AMITABHA,期刊：Journal of Medicinal Chemistry, 页码：7892-7896 , 文章类型： Article，,卷期：2009年52-23] A series of "long-chain" 1-(2-methoxyphenyl)piperzine derivatives containing an environment-sensitive fluorescent moiety (4-amino-1,8-naphthalimide, 4-dimethylaminophthalimide, dansyl) was synthesized. The compounds disp... Further Studies on Arylpiperazinyl Alkyl Pyridazinones: Discovery of an Exceptionally Potent, Orally Active, Antinociceptive Agent in Thermally Induced Pain [作者：BIANCALANI CLAUDIO; GIOVANNONI MARIA PAOLA; PIERETTI STEFANO; CESARI NICOLETTA; GRAZIANO ALESSIA; VERGELLI CLAUDIA; CILIBRIZZI AGOSTINO; DI GIANUARIO AMALIA; COLUCCI MARIANTONELLA; MANGANO GIORGINA; GARRONE BEATRICE; POLENZANI LORENZO; DAL PIAZ VITTORIO,期刊：Journal of Medicinal Chemistry, 页码：7397-7409 , 文章类型： Article，,卷期：2009年52-23] A number of pyridazinone derivatives bearing all arylpiperazinylalkyl chain were synthesized and tested icv in it model of acute nociception induced by thermal stimuli in mice (tail flick). The most interesting and poten... Synthesis and in Vitro Evaluation of N-Substituted Maleimide Derivatives as Selective Monoglyceride Lipase Inhibitors [作者：MATUSZAK NICOLAS; MUCCIOLI GIULIO G; LABAR GEOFFRAY; LAMBERT DIDIER M,期刊：Journal of Medicinal Chemistry, 页码：7410-7420 , 文章类型： Article，,卷期：2009年52-23] The endocannabinoid 2-arachidonoylglycerol (2-AG) plays a major role in many physiological processes, and its action is quickly terminated via enzymatic hydrolysis catalyzed by monoglyceride lipase (MGL). Regulating its ... Discovery of Trp-His and His-Arg Analogues as New Structural Classes of Short Antimicrobial Peptides [作者：SHARMA ROHIT K; REDDY RAVI P; TEGGE WERNER; JAIN RAHUL,期刊：Journal of Medicinal Chemistry, 页码：7421-7431 , 文章类型： Article，,卷期：2009年52-23] Naturally occurring antimicrobial peptides contain a large number of amino acid residues, which limits their clinical applicability. In search of short antimicrobial peptides, which represent a possible alternative for l... Synthesis and Biological Evaluation of 2-Alkynyl-N-6-methyl-5 '-N-methylcarboxamidoadenosine Derivatives as Potent and Highly Selective Agonists for the Human Adenosine A(3) Receptor [作者：VOLPINI ROSARIA; BUCCIONI MICHELA; DAL BEN DIEV; LAMBERTUCCI CATIA; LAMMI CARMEN; MARUCCI GABRIELLA; RAMADORI ANNA T; KLOTZ KARLNORBERT; CRISTALLI GLORIA,期刊：Journal of Medicinal Chemistry, 页码：7897-7900 , 文章类型： Article，,卷期：2009年52-23] A new series of 2-aralkynyl-N-6-methyl-MECAs 10-13 were synthesized and evaluated in radioligand binding studies and in a new Eu-GTP functional assay that provides a powerful alternative to radioisotope use. The new comp... Rapid Generation of a High Quality Lead for Transforming Growth Factor-beta (TGF-beta) Type I Receptor (ALK5) [作者：GOLDBERG FREDERICK W; WARD RICHARD A; POWELL STEVEN J; DEBRECZENI JUDIT E; NORMAN RICHARD A; ROBERTS NICOLA J; DISHINGTON ALLAN P; GINGELL HELEN J; WICKSON KATE F; ROBERTS ANDREW L,期刊：Journal of Medicinal Chemistry, 页码：7901-7905 , 文章类型： Article，,卷期：2009年52-23] A novel class of 4-pyridinoxy-2-anilinopyridine-based TGF-beta type I receptor (also known as activin-like kinase 5 or ALK5) inhibitors is reported. The binding mode of this scaffold was successfully predicted by analyzi... Vascular Disrupting Activity of Tubulin-Binding 1,5-Diaryl-1H-imidazoles [作者：BONEZZI KATIUSCIA; TARABOLETTI GIULIA; BORSOTTI PATRIZIA; BELLINA FABIO; ROSSI RENZO; GIAVAZZI RAFFAELLA,期刊：Journal of Medicinal Chemistry, 页码：7906-7910 , 文章类型： Article，,卷期：2009年52-23] Highly cytotoxic 1,5-diaryl-1H-imidazoles were studied to clarify the relationship between cytotoxicity and activity as vascular disrupting agents (VDA). All the compounds disorganized the tubulin cytoskeleton, affected ... Foreword: American Chemical Society Division of Medicinal Chemistry. Celebrating 100 Years of Excellence [作者：WOSTER PATRICK M,期刊：Journal of Medicinal Chemistry, 页码：7333-7338 , 文章类型： Editorial Material，,卷期：2009年52-23] Neglected Tropical Diseases: Multi-Target-Directed Ligands in the Search for Novel Lead Candidates against Trypanosoma and Leishmania [作者：CAVALLI ANDREA; BOLOGNESI MARIA LAURA,期刊：Journal of Medicinal Chemistry, 页码：7339-7359 , 文章类型： Review，,卷期：2009年52-23] Design, Synthesis, and Examination of Neuron Protective Properties of Alkenylated and Amidated Dehydro-Silybin Derivatives [作者：YANG LEI XIANG; HUANG KE XIN; LI HAI BO; GONG JING XU; WANG FENG; FENG YU BING; TAO QIAO FENG; WU YI HANG; LI XIAO KUN; WU XIU MEI; ZENG SU; SPENCER SHAWN; ZHAO YU; QU JIA,期刊：Journal of Medicinal Chemistry, 页码：7732-7752 , 文章类型： Review，,卷期：2009年52-23] A series of C7-O- and C20-O-amidated 2,3-dehydrosilybin (DHS) derivatives ((+/-)-1a-f and (+/-)-2), as well its it set of alkenylated DHS analogues ((+/-)-4a-f), were designed and de novo synthesized. A diesteric derivat... Nonpeptide Urotensin-II Receptor Antagonists: A New Ligand Class Based on Piperazino-Phthalimide and Piperazino-Isoindolinone Subunits [作者：LAWSON EDWARD C; LUCI DIANE K; GHOSH SHYAMALI; KINNEY WILLIAM A; REYNOLDS CHARLES H; QI JENSON; SMITH CHARLES E; WANG YUANPING; MINOR LISA K; HAERTLEIN BARBARA J; PARRY TOM J; DAMIANO BRUCE P; MARYANOFF BRUCE E,期刊：Journal of Medicinal Chemistry, 页码：7432-7445 , 文章类型： Article，,卷期：2009年52-23] We have discovered two related chemical series of nonpeptide urotensin-II (U-II) receptor antagonists based oil piperazino-phthalimide (5 and 6) and piperazino-isoindolinone (7) scaffolds. These structure types are disti... Discovery of Azetidinyl Ketolides for the Treatment of Susceptible and Multidrug Resistant Community-Acquired Respiratory Tract Infections [作者：MAGEE THOMAS V; RIPP SHARON L; LI BRYAN; BUZON RICHARD A; CHUPAK LOU; DOUGHERTY THOMAS J; FINEGAN STEVEN M; GIRARD DENNIS; HAGEN ANNE E; FALCONE MICHAEL J; FARLEY KATHLEEN A; GRANSKOG KARL; HARDINK JOEL R; HUBAND MICHAEL D; KAMICKER BARBARA J; KANEKO TAKUSHI; KNICKERBOCKER MICHAEL J; LIRAS JENNIFER L; MARRA ANDREA; MEDINA IVY; NGUYEN THUYTRINH; NOE MARK C; OBACH R SCOTT; ODONNELL JOHN P; PENZIEN JOSEPH B; REILLY USA DATTA; SCHAFER JOHN R; SHEN YUE; STONE GREGORY G; STRELEVITZ TIMOTHY J; SUN JIANMIN; TAITKAMRADT AMELIA; VAZ ALFIN D N; WHIPPLE DAVID A; WIDLICKA DANIEL W; WISHKA DONN G; WOLKOWSKI JOANNA P; FLANAGAN MARK E,期刊：Journal of Medicinal Chemistry, 页码：7446-7457 , 文章类型： Article，,卷期：2009年52-23] Respiratory tract bacterial strains are becoming increasingly resistant to currently marketed macrolide antibiotics. The current alternative telithromycin (1) from the newer ketolide class of macrolides addresses resista... Malaria-Infected Mice Live until at Least Day 30 after a New Monomeric Trioxane Combined with Mefloquine Are Administered Together in a Single Low Oral Dose [作者：WOODARD LAUREN E; CHANG WONSUK; CHEN XIAOCHUN; LIU JUN O; SHAPIRO THERESA A; POSNER GARY H,期刊：Journal of Medicinal Chemistry, 页码：7458-7462 , 文章类型： Article，,卷期：2009年52-23] In only five simple steps and 48% overall yield from the natural trioxane artemisinin, the thermally and hydrolytically stable trioxane fluoroanilide 4b has been prepared. Upon one oral dose of only 6.8 mg/kg of monomeri...