- Lipid-Lowering (Hetero)Aromatic Tetrahydro-1,4-Oxazine Derivatives with Antioxidant and Squalene Synthase Inhibitory Activity.
[作者:Kourounakis, Angeliki P.;Charitos, Christos;Rekka, Eleni A.;Kourounakis, Panos N.;,期刊:Journal of Medicinal Chemistry, 页码:5861-5865 , 文章类型: 研究论文,,卷期:2008年51-18]
- A no. of newly synthesized 2-[4-(hetero)arom.]phenyl-2-hydroxy-tetrahydro-1,4-oxazine derivs. as well as rat squalene synthase (IC50 for most between 1-10 mM). Antidyslipidemic action was demonstrated in vivo: the most a...
- Phosphate Prodrugs Derived from N-Acetylglucosamine Have Enhanced Chondroprotective Activity in Explant Cultures and Represent a New Lead in Antiosteoarthritis Drug Discovery.
[作者:McGuigan, Christopher;Serpi, Michaela;Bibbo, Rita;Roberts, Helen;Hughes, Clare;Caterson, Bruce;Gibert, Ana Torrent;Verson, Carlos Raul Alez;,期刊:Journal of Medicinal Chemistry, 页码:5807-5812 , 文章类型: 研究论文,,卷期:2008年51-18]
- We report the application of the phosphoramidate ProTide approach, developed by us for antiviral nucleosides, to sugar derivs. with potential chondro-protection against osteoarthritis. In particular, N-acetylglucosamine...
- Phosphoramidate Dinucleosides as Hepatitis C Virus Polymerase Inhibitors.
[作者:Zlatev, Ivan;Dutartre, Helene;Barvik, Ivan;Neyts, Johan;Canard, Bruno;Vasseur, Jean-Jacques;Alvarez, Karine;Morvan, Francois;,期刊:Journal of Medicinal Chemistry, 页码:5745-5757 , 文章类型: 研究论文,,卷期:2008年51-18]
- GC dinucleosides exhibiting a phosphoramidate internucleosidic linkage with neutral, amphiphile, pos. or neg. charged side chains were synthesized. Their potential inhibitory effect on the hepatitis C virus (HCV) NS5B p...
- A b-Fluoroamine Inhibitor of Purine Nucleoside Phosphorylase.
[作者:Mason, Jennifer M.;Murkin, Andrew S.;Li, Lei;Schramm, Vern L.;Gainsford, Graeme J.;Skelton, Brian W.;,期刊:Journal of Medicinal Chemistry, 页码:5880-5884 , 文章类型: 研究论文,,卷期:2008年51-18]
- The potent immucillin purine nucleoside phosphorylase (PNP) inhibitors F-DADMe-ImmH (3S,4S)-I and (3R,4R)-I are synthesized in seven steps. Cycloaddn. to a fluoroalkene and an enzymic resoln. are the key features of the...
- Synthesis and in Vitro Evaluation of 5-[18F]Fluoroalkyl Pyrimidine Nucleosides for Molecular Imaging of Herpes Simplex Virus Type 1 Thymidine Kinase Reporter Gene Expression.
[作者:Chacko, Ann-Marie;Qu, Wenchao;Kung, Hank F.;,期刊:Journal of Medicinal Chemistry, 页码:5690-5701 , 文章类型: 研究论文,,卷期:2008年51-18]
- Two novel series of 5-fluoroalkyl-2'-deoxyuridines I (R = H, x= 3, 4, 5) that have three, four, or five methylene units (Pr, Bu, or pentyl) at C-5 were prepd. and tested as reporter probes for imaging herpes simplex viru...
- Design, Synthesis, and Evaluation of Novel Organophosphorus Inhibitors of Bacterial Ureases.
[作者:Vassiliou, Stamatia;Grabowiecka, Agnieszka;Kosikowska, Paulina;Yiotakis, Athanasios;Kafarski, Pawel;Berlicki, Lukasz;,期刊:Journal of Medicinal Chemistry, 页码:5736-5744 , 文章类型: 研究论文,,卷期:2008年51-18]
- A new group of organophosphorus inhibitors of urease, P-Me phosphinic acids was discovered by using the structure based inhibitor design approach. Several derivs. of the lead compd., aminomethyl(methyl)phosphinic acid, ...
- 6-Azido-7-nitro-1,4-dihydroquinoxaline-2,3-dione (ANQX) Forms an Irreversible Bond To the Active Site of the GluR2 AMPA Receptor.
[作者:Cruz, Leslie A.;Estebanez-Perpina, Eva;Pfaff, Sam;Borngraeber, Sabine;Bao, Ning;Blethrow, Justin;Fletterick, Robert J.;England, Pamela M.;,期刊:Journal of Medicinal Chemistry, 页码:5856-5860 , 文章类型: 研究论文,,卷期:2008年51-18]
- essential for synaptic plasticity. ANQX, a photoreactive AMPA receptor antagonist, is an important biol. probe used to irreversibly inactivate AMPA receptors. Here, using X-ray crystallog. and mass spectroscopy, we rep...
- Melanocortin Tetrapeptide Ac-His-DPhe-Arg-Trp-NH2 Modified at the Para Position of the Benzyl Side Chain (DPhe): Importance for Mouse Melanocortin-3 Receptor Agonist versus Antagonist Activity.
[作者:Proneth, Bettina;Pogozheva, Irina D.;Portillo, Federico P.;Mosberg, Henry I.;Haskell-Luevano, Carrie;,期刊:Journal of Medicinal Chemistry, 页码:5585-5593 , 文章类型: 研究论文,,卷期:2008年51-18]
- The melanocortin-3 and -4 receptors (MC3R, MC4R) have been implicated in energy homeostasis and obesity. Whereas the physiol. role of the MC4R is extensively studied, little is known about the MC3R. One caveat is the li...
- Novel opioid peptide derived antagonists containing (2S)-2-methyl-3-(2,6-dimethyl-4-carbamoylphenyl)propanoic acid [(2S)-Mdcp].
[作者:Ghosh, Animesh;Luo, Jie;Liu, Chen;Weltrowska, Grazyna;Lemieux, Carole;Chung, Nga N.;Lu, Yixin;Schiller, Peter W.;,期刊:Journal of Medicinal Chemistry, 页码:5866-5870 , 文章类型: 研究论文,,卷期:2008年51-18]
- A synthesis of the novel tyrosine analog (2S)-2-methyl-3-(2,6-dimethyl-4-carbamoylphenyl)propanoic acid [(2S)-Mdcp] was developed. In (2S)-Mdcp, the amino and hydroxyl groups of 2',6'-dimethyltyrosine are replaced by a ...
- Oversulfated Chondroitin Sulfate: Impact of a Heparin Impurity, Associated with Adverse Clinical Events, on Low-Molecular-Weight Heparin Preparation.
[作者:Zhang, Zhenqing;Weiwer, Michel;Li, Boyangzi;Kemp, Melissa M.;Daman, Tyler H.;Linhardt, Robert J.;,期刊:Journal of Medicinal Chemistry, 页码:5498-5501 , 文章类型: 研究论文,,卷期:2008年51-18]
- Heparin, a widely used anticoagulant, is being rapidly displaced by low-mol.-wt. heparins. Recently, certain lots of heparin have been assocd. with anaphylactoid-type reactions resulting from contamination with oversulf...
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