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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39条记录   Thermodynamic and Structure Guided Design of Statin Based Inhibitors of 3-Hydroxy-3-Methylglutaryl Coenzyme A Reductase. [作者：Sarver, Ronald W.;Bills, Elizabeth;Bolton, Gary;Bratton, Larry D.;Caspers, Nicole L.;Dunbar, James B.;Harris, Melissa S.;Hutchings, Richard H.;Kennedy, Robert M.;Larsen, Scott D.;Pavlovsky, Alexander;Pfefferkorn, Jeffrey A.;Bainbridge, Graeme;,期刊：Journal of Medicinal Chemistry, 页码：3804-3813 , 文章类型： 研究论文，,卷期：2008年51-13] Clin. studies have demonstrated that statins, 3-hydroxy-3-methylglutaryl CoA reductase (HMGR) inhibitors, are effective at lowering mortality levels assocd. with cardiovascular disease; however, 2-7% of patients may expe... Selective Influence on Contextual Memory: Physiochemical Properties Associated with Selectivity of Benzodiazepine Ligands at GABAA Receptors Containing the a5 Subunit. [作者：Harris, Danni;Clayton, Terry;Cook, James;Sahbaie, Peyman;Halliwell, Robert F.;Furtmuller, Roman;Huck, Sigismund;Sieghart, Werner;DeLorey, Timothy M.;,期刊：Journal of Medicinal Chemistry, 页码：3788-3803 , 文章类型： 研究论文，,卷期：2008年51-13] Ligands that bind to the benzodiazepine binding site on the GABAA receptor can attenuate or potentiate cognition. To investigate this property, the chem. determinants favoring selective binding or selective activation o... Efficient Synthesis and Neuroprotective Effect of Substituted 1,3-Diphenyl-2-propen-1-ones. [作者：Jung, Jae-Chul;Jang, Soyong;Lee, Yongnam;Min, Dongguk;Lim, Eunyoung;Jung, Heyin;Oh, Miyeon;Oh, Seikwan;Jung, Mankil;,期刊：Journal of Medicinal Chemistry, 页码：4054-4058 , 文章类型： 研究论文，,卷期：2008年51-13] 1, 22 An efficient synthesis involving a key aldol reaction and biol. properties of a series of 1,3-diphenyl-2-propen-1-ones is described. The in vitro activity for 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavengin... Hydrochalarones: A Novel Endohedral Metallofullerene Platform for Enhancing Magnetic Resonance Imaging Contrast. [作者：MacFarland, Darren K.;Walker, Kenneth L.;Lenk, Robert P.;Wilson, Stephen R.;Kumar, Krishan;Kepley, Christopher L.;Garbow, Joel R.;,期刊：Journal of Medicinal Chemistry, 页码：3681-3683 , 文章类型： 研究论文，,卷期：2008年51-13] vasculature for extended periods of time. A new contrast agent is described in which gadolinium is encapsulated within an extremely stable carbon sphere, thus allowing for safe extended residence. Water soly. and small ... Characterization of the Drug Binding Specificity of Rat Liver Fatty Acid Binding Protein. [作者：Chuang, Sara;Velkov, Tony;Horne, James;Porter, Christopher J. H.;Scanlon, Martin J.;,期刊：Journal of Medicinal Chemistry, 页码：3755-3764 , 文章类型： 研究论文，,卷期：2008年51-13] Liver-fatty acid binding protein (L-FABP) is found in high levels in enterocytes and is involved in the cytosolic solubilization of fatty acids during fat absorption. In the current studies, the interaction of L-FABP wi... A Tissue-Selective Nonsteroidal Progesterone Receptor Modulator: 7,9-Difluoro-5-(3-methylcyclohex-2-enyl)-2,2,4-trimethyl-1,2-dihydrochro meno[3,4-f]quinoline. [作者：Pedram, Bijan;van Oeveren, Arjan;Mais, Dale E.;Marschke, Keith B.;Verbost, Pieter M.;Groen, Marinus B.;Zhi, Lin;,期刊：Journal of Medicinal Chemistry, 页码：3696-3699 , 文章类型： 研究论文，,卷期：2008年51-13] The progesterone receptor plays an important role in the female reproductive system. Here the authors describe the discovery of a new selective progesterone receptor modulator (SPRM). In rats, the lead compd. (I), inhi... Modulation of Peripheral Serotonin Levels by Novel Tryptophan Hydroxylase Inhibitors for the Potential Treatment of Functional Gastrointestinal Disorders. [作者：Shi, Zhi-Cai;Devasagayaraj, Arokiasamy;Gu, Kunjian;Jin, Haihong;Marinelli, Brett;Samala, Lakshman;Scott, Sheldon;Stouch, Terry;Tunoori, Ashok;Wang, Ying;Zang, Yi;Zhang, Chengmin;Kimball, S. David;Main, Alan J.;Sun, Weimei;Yang, Qi;Nouraldeen, Amr;Yu, Xian,期刊：Journal of Medicinal Chemistry, 页码：3684-3687 , 文章类型： 研究论文，,卷期：2008年51-13] (TPH) inhibitors is described. This class of TPH inhibitors exhibits excellent potency in in vitro biochem. and cell-based assays, and it selectively reduces serotonin levels in the murine intestine after oral administr... 7-Aminopyrazolo[1,5-a]pyrimidines as Potent Multitargeted Receptor Tyrosine Kinase Inhibitors. [作者：Frey, Robin R.;Curtin, Michael L.;Albert, Daniel H.;Glaser, Keith B.;Pease, Lori J.;Soni, Niru B.;Bouska, Jennifer J.;Reuter, David;Stewart, Kent D.;Marcotte, Patrick;Bukofzer, Gail;Li, Junling;Davidsen, Steven K.;Michaelides, Michael R.;,期刊：Journal of Medicinal Chemistry, 页码：3777-3787 , 文章类型： 研究论文，,卷期：2008年51-13] 7-Aminopyrazolo[1,5-a]pyrimidine urea receptor tyrosine kinase inhibitors have been discovered. Investigation of structure-activity relationships of the pyrazolo[1,5-a]pyrimidine nucleus led to a series of 6-(4-N,N'-dip... The Micelle-Associated 3D Structures of Boc-Y(SO3)-Nle-G-W-Nle-D-2-phenylethylester (JMV-180) and CCK-8(s) Share Conformational Elements of a Calculated CCK1 Receptor-Bound Model. [作者：Kumar, Mohanraja;Reeve, Joseph R.;Hu, Weidong;Miller, Laurence J.;Keire, David A.;,期刊：Journal of Medicinal Chemistry, 页码：3742-3754 , 文章类型： 研究论文，,卷期：2008年51-13] JMV-180 (1) and CCK-8(s) are high affinity ligands at the CCK1 receptor that have similar and different actions via this receptor. Here we calc. the tertiary structure of 1 or CCK-8(s) in the presence of dodecylphosphoc... Interaction of Methimazole with I2: X-ray Crystal Structure of the Charge Transfer Complex Methimazole-I2. Implications for the Mechanism of Action of Methimazole-Based Antithyroid Drugs. [作者：Isaia, Francesco;Aragoni, M. Carla;Arca, Massimiliano;Demartin, Francesco;Devillanova, Francesco A.;Floris, Giovanni;Garau, Alessandra;Hursthouse, Michael B.;Lippolis, Vito;Medda, Rosaria;Oppo, Fabio;Pira, Marilena;Verani, Gaetano;,期刊：Journal of Medicinal Chemistry, 页码：4050-4053 , 文章类型： 研究论文，,卷期：2008年51-13] in a multistep process, 1-methylimidazole as final product. In this process, the charge transfer complex MMI-I2 and the ionic disulfide [(C4H6N2S-)2]2+ (1, dication MMI disulfide) have been isolated and their x-ray crys... Synthesis, Biological Activity, and Structure-Activity Relationships for Potent Cytotoxic Rhodium(III) Polypyridyl Complexes. [作者：Harlos, Melanie;Ott, Ingo;Gust, Ronald;Alborzinia, Hamed;Wolfl, Stefan;Kromm, Anna;Sheldrick, William S.;,期刊：Journal of Medicinal Chemistry, 页码：3924-3933 , 文章类型： 研究论文，,卷期：2008年51-13] Mer-[RhCl3(DMSO-kS)(pp)] (1a-5a) may be prepd. by reaction of mer,cis-[RhCl3(DMSO-kS)2(DMSO-kO)] with the appropriate polypyridyl ligand (pp = bpy, phen, dpq, dppz, dppn) in MeOH/water soln. at 75? The mer isomers of 1a... 1-[(3-Aryloxy-3-aryl)propyl]-1H-imidazoles, New Imidazoles with Potent Activity against Candida albicans and Dermatophytes. Synthesis, Structure-Activity Relationship, and Molecular Modeling Studies. [作者：La Regina, Giuseppe;Diodata D'Auria, Felicia;Tafi, Andrea;Piscitelli, Francesco;Olla, Stefania;Caporuscio, Fabiana;Nencioni, Lucia;Cirilli, Roberto;La Torre, Francesco;Rodrigues De Melo, Nadja;Kelly, Steven L.;Lamb, David C.;Artico, Marino;Botta, Maurizio,期刊：Journal of Medicinal Chemistry, 页码：3841-3855 , 文章类型： 研究论文，,卷期：2008年51-13] New 1-[(3-aryloxy-3-aryl)propyl]-1H-imidazoles, e.g. I [R1 = H, 4-Cl, 4-F, 4-Me, R2 = H, 4-CL, 4-Me, 2,4-Cl2, 3,5-Cl2, X = CH, Y = (CH2)n, n= 2], were synthesized and evaluated against Candida albicans and dermatophytes ... Design, Synthesis, and Biological Evaluation of Novel 3-Aryl-4-(1H-indol-3-yl)-1,5-dihydro-2H-pyrrol-2-ones as Vascular Endothelial Growth Factor Receptor (VEGF-R) Inhibitors. [作者：Peifer, Christian;Selig, Roland;Kinkel, Katrin;Ott, Dimitri;Totzke, Frank;Schaechtele, Christoph;Heidenreich, Regina;Roecken, Martin;Schollmeyer, Dieter;Laufer, Stefan;,期刊：Journal of Medicinal Chemistry, 页码：3814-3824 , 文章类型： 研究论文，,卷期：2008年51-13] In this study we report on the design, synthesis, and biol. evaluation of pyrrol-2-one I (X = C:O, Y = CH2) (II) to be a highly potent VEGF-R2/3 inhibitor with IC50 of 31/37 nM. The novel 3,4-diaryl-2H-pyrrol-2-ones wer... Novel g-aminobutyric acid r1 receptor antagonists; synthesis, pharmacological activity and structure-activity relationships. [作者：Kumar, Rohan J.;Chebib, Mary;Hibbs, David E.;Kim, Hye-Lim;Johnston, Graham A. R.;Salam, Noeris K.;Hanrahan, Jane R.;,期刊：Journal of Medicinal Chemistry, 页码：3825-3840 , 文章类型： 研究论文，,卷期：2008年51-13] g-Aminobutyric acid (GABA) phosphinic acid analogs, (4-amino-1-cyclopenten-1-yl)-R-phosphinic acids (34-42; R = Me, Et, iPr, Bu, PhCH2), (3-amino-1-hydroxycyclobutyl)(methyl)phosphinic acids (51, 52) and (3-aminocyclobut... Design, Synthesis, and Testing of Non-Nephrotoxic Desazadesferrithiocin Polyether Analogues. [作者：Bergeron, Raymond J.;Wiegand, Jan;McManis, James S.;Bharti, Neelam;Singh, Shailendra;,期刊：Journal of Medicinal Chemistry, 页码：3913-3923 , 文章类型： 研究论文，,卷期：2008年51-13] A series of iron-clearing efficiencies (ICEs), ferrokinetics, and toxicity studies for (S)-2-(2,4-dihydroxyphenyl)-4,5-dihydro-4-methyl-4-thiazolecarboxylic acid (deferitrin, 1), (S)-4,5-dihydro-2-[2-hydroxy-4-(3,6,9-tri... Design, Synthesis, and Evaluation of Novel Mutual Prodrugs (Hybrid Drugs) of All-trans-Retinoic Acid and Histone Deacetylase Inhibitors with Enhanced Anticancer Activities in Breast and Prostate Cancer Cells in Vitro. [作者：Gediya, Lalji K.;Khandelwal, Aakanksha;Patel, Jyoti;Belosay, Aashvini;Sabnis, Gauri;Mehta, Jhalak;Purushottamachar, Puranik;Njar, Vincent C. O.;,期刊：Journal of Medicinal Chemistry, 页码：3895-3904 , 文章类型： 研究论文，,卷期：2008年51-13] Novel mutual prodrugs (MPs) of ATRA (all-trans-retinoic acid) and HDIs (histone deacetylase inhibitors) (10, 13, 17-19) connected via glycine acyloxyalkyl carbamate linker (AC linker) or through a benzyl ester linker (1,...