Search Results - "Bourguignon, JJ"

Regiospecific thermal C-acylation of imidazo [1,2-a] pyridines via an N-acylimidazolium intermediate by Chayer, Saïd, Schmitt, Martine, Collot, Valérie, Bourguignon, Jean-Jacques

“…Direct acylation of imidazo [1,2-a] pyridines in a sealed tube at 130°C and without catalyst gave various 3-acyl derivatives in satisfactory yields. Acylation…”
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Involvement of neuropeptide FF receptors in neuroadaptive responses to acute and chronic opiate treatments by Elhabazi, K, Trigo, JM, Mollereau, C, Moulédous, L, Zajac, J‐M, Bihel, F, Schmitt, M, Bourguignon, JJ, Meziane, H, Petit‐demoulière, B, Bockel, F, Maldonado, R, Simonin, F

“…BACKGROUND AND PURPOSE Opiates remain the most effective compounds for alleviating severe pain across a wide range of conditions. However, their use is…”
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Aminoguanidine Hydrazone Derivatives as Nonpeptide NPFF1 Receptor Antagonists Reverse Opioid Induced Hyperalgesia by Hammoud, Hassan, Elhabazi, Khadija, Quillet, Raphäelle, Bertin, Isabelle, Utard, Valérie, Laboureyras, Emilie, Bourguignon, Jean-Jacques, Bihel, Frédéric, Simonnet, Guy, Simonin, Frédéric, Schmitt, Martine

“…Neuropeptide FF receptors (NPFF1R and NPFF2R) and their endogenous ligand neuropeptide FF have been shown previously to display antiopioid properties and to…”
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RF9, a Potent and Selective Neuropeptide FF Receptor Antagonist, Prevents Opioid-Induced Tolerance Associated with Hyperalgesia by Simonin, Frédéric, Schmitt, Martine, Laulin, Jean-Paul, Laboureyras, Emilie, Jhamandas, Jack H., MacTavish, David, Matifas, Audrey, Mollereau, Catherine, Laurent, Patrick, Parmentier, Marc, Kieffer, Brigitte L., Bourguignon, Jean-Jacques, Simonnet, Guy

“…Neuropeptide FF (NPFF) has been proposed to play a role in pain modulation, opioid tolerance, and several other physiological processes. However,…”
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Fluorescent Derivatives of the GFP Chromophore Give a New Insight into the GFP Fluorescence Process by Follenius-Wund, Anny, Bourotte, Maryline, Schmitt, Martine, Iyice, Fatih, Lami, Hans, Bourguignon, Jean-Jacques, Haiech, Jacques, Pigault, Claire

“…The photophysical properties of synthetic compounds derived from the imidazolidinone chromophore of the green fluorescent protein were determined. Various…”
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Design of Small-Sized Libraries by Combinatorial Assembly of Linkers and Functional Groups to a Given Scaffold: Application to the Structure-Based Optimization of a Phosphodiesterase 4 Inhibitor by Krier, Mireille, de Araújo-Júnior, João X, Schmitt, Martine, Duranton, Jérôme, Justiano-Basaran, Hélène, Lugnier, Claire, Bourguignon, Jean-Jacques, Rognan, Didier

“…Combinatorial chemistry and library design have been reconciled by applying simple medicinal chemistry concepts to virtual library design. The herein reported…”
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Aminopyridazines as Acetylcholinesterase Inhibitors by Contreras, Jean-Marie, Rival, Yveline M, Chayer, Said, Bourguignon, Jean-Jacques, Wermuth, Camille G

“…Following the discovery of the weak, competitive and reversible acetylcholinesterase (AChE)-inhibiting activity of minaprine (3c) (IC50 = 85 μM on homogenized…”
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Iminoiodane mediated aziridination of α-allylglycine: access to a novel rigid arginine derivative and to the natural amino acid enduracididine by Sanière, Laurent, Leman, Loı̈c, Bourguignon, Jean-Jacques, Dauban, Philippe, Dodd, Robert H

“…The synthesis of fully protected aminodihydrohistidines in optically pure form is described starting from allylglycine derivatives. These compounds represent…”
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A general approach toward the synthesis of C-nucleoside pyrazolo[1,5-a]-1,3,5-triazines and their 3',5'-bisphosphate C-nucleotide analogues as the first reported in vivo stable P2Y(1)-receptor antagonists by Raboisson, Pierre, Baurand, Anthony, Cazenave, Jean-Pierre, Gachet, Christian, Schultz, Dominique, Spiess, Bernard, Bourguignon, Jean-Jacques

“…In our effort to identify potent purinergic P2Y(1) receptor antagonists as potent platelet aggregation inhibitors with enhanced metabolic stability, we…”
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Fluorophores related to the green fluorescent protein by Bourotte, Maryline, Schmitt, Martine, Follenius-Wund, Anny, Pigault, Claire, Haiech, Jacques, Bourguignon, Jean-Jacques

“…Graphic Imidazolin-5-one derivatives and isosteres (oxazolinones, butenolides, and pyrrolinones) of the 4-hydroxybenzylidene-imidazolinone chromophore of the…”
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Fluorescence resonance energy transfer to probe human M1 muscarinic receptor structure and drug binding properties by Ilien, Brigitte, Franchet, Christelle, Bernard, Philippe, Morisset, Séverine, Odile Weill, Claire, Bourguignon, Jean‐Jacques, Hibert, Marcel, Galzi, Jean‐Luc

“…Human M1 muscarinic receptor chimeras were designed (i) to allow detection of their interaction with the fluorescent antagonist pirenzepine labelled with…”
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Synthesis and biological activity of 2-alkylated deoxyadenosine bisphosphate derivatives as P2Y(1) receptor antagonists by Mathieu, Romain, Baurand, Anthony, Schmitt, Martine, Gachet, Christian, Bourguignon, Jean-Jacques

“…A previous study around adenine nucleotides afforded the reference N(6)-methyl-2'-deoxyadenosine-3',5'-bisphosphate (1a, MRS 2179) as a selective human P2Y(1)…”
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Discovery of a 3-Amino-6-phenyl-pyridazine Derivative as a New Synthetic Antineuroinflammatory Compound by Mirzoeva, Salida, Sawkar, Anu, Zasadzki, Magdalena, Guo, Ling, Velentza, Anastasia V, Dunlap, Vincent, Bourguignon, Jean-Jacques, Ramstrom, Helena, Haiech, Jacques, Van Eldik, Linda J, Watterson, D. Martin

“…Excessive glial activation, with overproduction of cytokines and oxidative stress products, is detrimental and a hallmark of neurodegenerative disease…”
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Mapping and Fitting the Peripheral Benzodiazepine Receptor Binding Site by Carboxamide Derivatives. Comparison of Different Approaches to Quantitative Ligand−Receptor Interaction Modeling by Anzini, Maurizio, Cappelli, Andrea, Vomero, Salvatore, Seeber, Michele, Menziani, Maria Cristina, Langer, Thierry, Hagen, Bertram, Manzoni, Cristina, Bourguignon, Jean-Jacques

“…The synthetic-computational approach to the study of the binding site of peripheral benzodiazepine receptor (PBR) ligands related to…”
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Heterocyclic Bis-Cations as Starting Hits for Design of Inhibitors of the Bifunctional Enzyme Histidine-Containing Protein Kinase/Phosphatase from Bacillus subtilis by RAMSTRöM, Helena, BOUROTTE, Maryline, PHILIPPE, Claude, SCHMITT, Martine, HAIECH, Jacques, BOURGUIGNON, Jean-Jacques

“…The main mechanism of carbon catabolite repression/activation in low-guanine and low-cytosine Gram-positive bacteria seems to involve phosphorylation of HPr…”
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New strategies towards proline derivatives as conformationally constrained arginine analogues by Pellegrini, Nadia, Schmitt, Martine, Guery, Sébastien, Bourguignon, Jean-Jacques

“…The cyano derivatives of 3-functionalized dehydroprolines led to arginine semi–constrained analogues. Preparation of cis and trans 3-substituted prolines as…”
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Isolation and NMR characterization of the indolomonoterpenoid alkaloids from Aspidosperma pyrifolium by Araujo-Junior X.J., De, Antheaume, C., Trindade, C., Schmitt, M., Jj, Bourguignon, A.E.G., Santana

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Rapid access to cis 3-substituted prolines by Pellegrini, Nadia, Schmitt, Martine, Bourguignon, Jean-Jacques

“…The O-triflate of 2-cyano-3-oxopyrrolidine was obtained and used in a palladium coupling reaction. The resulting Δ 2-pyrrolidine derivatives allowed…”
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Design, synthesis and structure–activity relationships of a series of 9-substituted adenine derivatives as selective phosphodiesterase type-4 inhibitors by Raboisson, Pierre, Lugnier, Claire, Muller, Christian, Reimund, Jean-Marie, Schultz, Dominique, Pinna, Guillaume, Le Bec, Alain, Basaran, Hélène, Desaubry, Laurent, Gaudiot, François, Seloum, Mohamed, Bourguignon, Jean-Jacques

“…Adenine derivatives substituted in position 9 have been demonstrated to have potent cyclic nucleotide phosphodiesterase (PDE) inhibition properties with high…”
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Efficient synthesis of 8-substituted pyrazolo[1,5- a]-1,3,5-triazines by regioselective acylation by Raboisson, Pierre, Schultz, Dominique, Lugnier, Claire, Bourguignon, Jean-Jacques

“…An efficient two-step synthesis of 8-acylated pyrazolo[1,5- a]-1,3,5-triazines has been accomplished. The key strategic elements of this novel synthetic…”
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