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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21条记录   Physicochemical properties of antibacterial compounds: implications for drug discovery. [作者：O'Shea, Rosemarie;Moser, Heinz E.;,期刊：Journal of Medicinal Chemistry, 页码：2871-2878 , 文章类型： 研究论文，,卷期：2008年51-10] With the rise of multidrug-resistant pathogens and the need for novel antibiotics, it is crit. to understand as much as possible from prior efforts and to apply learned lessons to the discovery of future antibiotics. On... Discovery of Potent, Orally Bioavailable, Selective 5-HT1A/B/D Receptor Antagonists. [作者：Ward, Simon E.;Eddershaw, Peter J.;Scott, Claire M.;Gordon, Laurie J.;Lovell, Peter J.;Moore, Susan H.;Smith, Paul W.;Starr, Kathryn R.;Thewlis, Kevin M.;Watson, Jeannette M.;,期刊：Journal of Medicinal Chemistry, 页码：2887-2890 , 文章类型： 研究论文，,卷期：2008年51-10] 5-HT1 receptor antagonists have been discovered with good selectivity over the 5-HT transporter. This is the first report of highly potent, selective ligands for the 5-HT1A/B/D receptors with low intrinsic activity, whi... Aminoacyl-tRNA Synthetase Inhibitors as Potent and Synergistic Immunosuppressants. [作者：Van de Vijver, Pieter;Ostrowski, Tomasz;Sproat, Brian;Goebels, Jozef;Rutgeerts, Omer;Van Aerschot, Arthur;Waer, Mark;Herdewijn, Piet;,期刊：Journal of Medicinal Chemistry, 页码：3020-3029 , 文章类型： 研究论文，,卷期：2008年51-10] The aminoacyl-tRNA synthetase family of enzymes is the target of many antibacterials and inhibitors of eukaryotic hyperproliferation. In screening analogs of 5'-O-(N-L-aminoacyl)-sulfamoyladenosine contg. all 20 protein... On the Applicability of GPCR Homology Models to Computer-Aided Drug Discovery: A Comparison between In Silico and Crystal Structures of the b2-Adrenergic Receptor. [作者：Costanzi, Stefano;,期刊：Journal of Medicinal Chemistry, 页码：2907-2914 , 文章类型： 研究论文，,卷期：2008年51-10] (b2-AR) proved that G protein-coupled receptors (GPCRs) share a structurally conserved rhodopsin-like 7TM core. Here, to probe to which extent realistic GPCR structures can be recreated through modeling, carazolol was d... 2-Amino-1,3-thiazol-4(5H)-ones as Potent and Selective 11b-Hydroxysteroid Dehydrogenase Type 1 Inhibitors: Enzyme-Ligand Co-Crystal Structure and Demonstration of Pharmacodynamic Effects in C57Bl/6 Mice. [作者：Johansson, Lars;Fotsch, Christopher;Bartberger, Michael D.;Castro, Victor M.;Chen, Michelle;Emery, Maurice;Gustafsson, Sonja;Hale, Clarence;Hickman, Dean;Homan, Evert;Jordan, Steven R.;Komorowski, Renee;Li, Aiwen;McRae, Kenneth;Moniz, George;Matsumoto, Gu,期刊：Journal of Medicinal Chemistry, 页码：2933-2943 , 文章类型： 研究论文，,卷期：2008年51-10] considerable attention during the past few years as a potential target for the treatment of diseases assocd. with metabolic syndrome. In the ongoing work on 11b-HSD1 inhibitors, a series of new 2-amino-1,3-thiazol-4(5H)... Bioisosteric Heterocyclic Versions of 7-{[2-(4-Phenyl-piperazin-1-yl)ethyl]propylamino}-5,6,7,8-tetrahydronap hthalen-2-ol: Identification of Highly Potent and Selective Agonists for Dopamine D3 Receptor with Potent in Vivo Activity. [作者：Biswas, Swati;Hazeldine, Stuart;Ghosh, Balaram;Parrington, Ingrid;Kuzhikandathil, Eldo;Reith, Maarten E. A.;Dutta, Aloke K.;,期刊：Journal of Medicinal Chemistry, 页码：3005-3019 , 文章类型： 研究论文，,卷期：2008年51-10] In the current report, the authors extend the SAR study on the hybrid structure 7-{[2-(4-phenyl-piperazin-1-yl)ethyl]propylamino}-5,6,7,8-tetrahydronaph thalen-2-ol further to include heterocyclic bioisosteric analogs. ... Thiocamptothecin. [作者：Samori, Cristian;Guerrini, Andrea;Varchi, Greta;Zunino, Franco;Beretta, Giovanni Luca;Femoni, Cristina;Bombardelli, Ezio;Fontana, Gabriele;Battaglia, Arturo;,期刊：Journal of Medicinal Chemistry, 页码：3040-3044 , 文章类型： 研究论文，,卷期：2008年51-10] The synthesis and the X-ray structure of 16a-thiocamptothecin (TCPT; I), the thiopyridone analog of camptothecin (CPT), are accomplished. The crystal contains two structurally identical, yet independent mols. Both of the... Spiro[(dihydropyrazin-2,5-dione)-6,3'-(2',3'-dihydrothieno[2,3-b]naphtho -4',9'-dione)]-Based Cytotoxic Agents: Structure-Activity Relationship Studies on the Substituent at N4-Position of the Diketopiperazine Domain. [作者：Gomez-Monterrey, Isabel;Campiglia, Pietro;Carotenuto, Alfonso;Stiuso, Paola;Bertamino, Alessia;Sala, Marina;Aquino, Claudio;Grieco, Paolo;Morello, Silvana;Pinto, Aldo;Ianelli, Pio;Novellino, Ettore;,期刊：Journal of Medicinal Chemistry, 页码：2924-2932 , 文章类型： 研究论文，,卷期：2008年51-10] Analogs of the previously reported potent cytotoxic spiro[(dihydropyrazine-2,5-dione)-6,3'-(2',3'-dihydrothieno[2,3-b]naphth o-4',9'-dione)] derivs. were prepd. to explore new structural requirements at the diketopiperaz... Benzofuran-Based Hybrid Compounds for the Inhibition of Cholinesterase Activity, b Amyloid Aggregation, and Ab Neurotoxicity. [作者：Rizzo, Stefano;Riviere, Celine;Piazzi, Lorna;Bisi, Alessandra;Gobbi, Silvia;Bartolini, Manuela;Andrisano, Vincenza;Morroni, Fabiana;Tarozzi, Andrea;Monti, Jean-Pierre;Rampa, Angela;,期刊：Journal of Medicinal Chemistry, 页码：2883-2886 , 文章类型： 研究论文，,卷期：2008年51-10] The complex etiol. of Alzheimer's disease (AD) prompts scientists to develop multitarget strategies to combat causes and symptoms. We therefore designed, synthesized, and tested new hybrid mols. I (R = H, COMe, COPh, et... Straightforward Recursive Partitioning Model for Discarding Insoluble Compounds in the Drug Discovery Process. [作者：Lamanna, Claudia;Bellini, Marta;Padova, Alessandro;Westerberg, Goran;Maccari, Laura;,期刊：Journal of Medicinal Chemistry, 页码：2891-2897 , 文章类型： 研究论文，,卷期：2008年51-10] Poor aq. soly. is one of the major issues in drug discovery and development, impacting neg. on all aspects of the research and development process. The pharmaceutical industry has realized that soly. issues need to be r... In vitro and in vivo evaluation of bifunctional bisthiosemicarbazone 64Cu-complexes for the positron emission tomography imaging of hypoxia. [作者：Bonnitcha, Paul D.;Vavere, Amy L.;Lewis, Jason S.;Dilworth, Jonathan R.;,期刊：Journal of Medicinal Chemistry, 页码：2985-2991 , 文章类型： 研究论文，,卷期：2008年51-10] The copper(II) bisthiosemicarbazonato complex, copper-diacetyl-bis(N4-methylthiosemicarbazonate) (Cu-ATSM), has been used clin. as a positron emission tomog. (PET) tracer for the derived from diacetyl-2-(4-N-methyl-3-thi... Structural Origin of Selectivity in Class II-Selective Histone Deacetylase Inhibitors. [作者：Estiu, Guillermina;Greenberg, Edward;Harrison, Christopher B.;Kwiatkowski, Nicholas P.;Mazitschek, Ralph;Bradner, James E.;Wiest, Olaf;,期刊：Journal of Medicinal Chemistry, 页码：2898-2906 , 文章类型： 研究论文，,卷期：2008年51-10] The development of class- and isoform-selective histone deacetylase (HDAC) inhibitors is highly desirable for the study of the complex interactions of these proteins central to transcription regulation as well as for the... Structure-Activity Relationship Studies on N'-Aryl Carbohydrazide P2X7 Antagonists. [作者：Nelson, Derek W.;Sarris, Kathy;Kalvin, Douglas M.;Namovic, Marian T.;Grayson, George;Donnelly-Roberts, Diana L.;Harris, Richard;Honore, Prisca;Jarvis, Michael F.;Faltynek, Connie R.;Carroll, William A.;,期刊：Journal of Medicinal Chemistry, 页码：3030-3034 , 文章类型： 研究论文，,卷期：2008年51-10] Structure-activity relationship (SAR) studies evaluated functional activity by monitoring calcium flux inhibition in cell lines expressing recombinant human and rat P2X7 receptors. Selected analogs were assayed in vitro... 4-Benzyl-1H-imidazoles with Oxazoline Termini as Histamine H3 Receptor Agonists. [作者：Wijtmans, Maikel;Celanire, Sylvain;Snip, Erwin;Gillard, Michel R.;Gelens, Edith;Collart, Philippe P.;Venhuis, Bastiaan J.;Christophe, Bernard;Hulscher, Saskia;van der Goot, Henk;Lebon, Florence;Timmerman, Henk;Bakker, Remko A.;Lallemand, Benedicte I. L. F,期刊：Journal of Medicinal Chemistry, 页码：2944-2953 , 文章类型： 研究论文，,卷期：2008年51-10] Research on the therapeutic applications of the histamine H3 receptor (H3R) has traditionally focused on antagonists/inverse agonists. In contrast, H3R agonists have received less attention despite their potential use i... From the Selective Serotonin Transporter Inhibitor Citalopram to the Selective Norepinephrine Transporter Inhibitor Talopram: Synthesis and Structure-Activity Relationship Studies. [作者：Eildal, Jonas N. N.;Andersen, Jacob;Kristensen, Anders S.;Jorgensen, Anne Marie;Bang-Andersen, Benny;Jorgensen, Morten;Stromgaard, Kristian;,期刊：Journal of Medicinal Chemistry, 页码：3045-3048 , 文章类型： 研究论文，,卷期：2008年51-10] Citalopram and talopram are structurally closely related, but they have very distinct pharmacol. profiles as selective inhibitors of the serotonin and norepinephrine transporters, resp. A systematic structure-activity r... Discovery and Optimization of Triazolopyridazines as Potent and Selective Inhibitors of the c-Met Kinase. [作者：Albrecht, Brian K.;Harmange, Jean-Christophe;Bauer, David;Berry, Loren;Bode, Christiane;Boezio, Alessandro A.;Chen, April;Choquette, Deborah;Dussault, Isabelle;Fridrich, Cary;Hirai, Satoko;Hoffman, Doug;Larrow, Jay F.;Kaplan-Lefko, Paula;Lin, Jasmine;Lohm,期刊：Journal of Medicinal Chemistry, 页码：2879-2882 , 文章类型： 研究论文，,卷期：2008年51-10] Tumorigenesis is a multistep process in which oncogenes play a key role in tumor formation, growth, and maintenance. MET was discovered as an oncogene that is activated by its ligand, hepatocyte growth factor. Deregula...