Zobrazeno 1 - 7
of 7
pro vyhledávání: '"Sabine, Defays"'
Autor:
Ingrid P. Buchler, Noelle White, Florian Montel, Florence Moureau, Gregory V. Carr, Thierry Demaude, Véronique Durieu, Daniel Akuma, James C. Barrow, Pablo De León, Martyn D. Wood, Nathalie Van houtvin, Vinh Au, Huijun Wei, Marie Christine Vandergeten, Emilie Jigorel, Yifang Huang, Dominique Swinnen, Anna Kolobova, Michael S. Poslusney, Martha Kimos, Glen Ernst, Michael DePasquale, Spencer Byers, Sabine Defays
Publikováno v:
ACS Medicinal Chemistry Letters
A series of bicyclic pyridones were identified as potent inhibitors of catechol O-methyltransferase (COMT). Substituted benzyl groups attached to the basic nitrogen of the core scaffold gave the most potent inhibitors within this series. Rat pharmaco
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f9cf6bbaad26b38d002dd4bc88ec3368
https://pubmed.ncbi.nlm.nih.gov/32038769
https://pubmed.ncbi.nlm.nih.gov/32038769
Autor:
Sylvain Celanire, Thierry Demaude, Laurent Provins, Yves Lamberty, Marie-Laure Delporte, Nathalie Van houtvin, Geneviève Lorent, Véronique Durieu, Sabine Defays, Frédéric Denonne, Michel Gillard, Bernard Christophe, Anne Valade, Alain Vanbellinghen, Delphine Hubert, Christel Delaunoy
Publikováno v:
ChemMedChem. 7:2087-2092
The simpler, the better: H(3) histamine receptor (H(3)R) are of interest as therapeutic targets in cognitive and somnolence disorders. Here, lead optimization of H(3)R inverse agonists bearing a thiazolo[5,4-c]piperidine group gave rise to a clinical
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::df1c8a01dc9993b1a09cf14ce69fe7dd
https://doi.org/10.1002/cmdc.201200406
https://doi.org/10.1002/cmdc.201200406
Autor:
Laurent Provins, Michel Gillard, Christel Delaunoy, Frédéric Denonne, Sabine Defays, Jean-Marie Nicolas, Geneviève Lorent, Eric Detrait, Véronique Durieu, Bernard Christophe, Yves Lamberty, Alain Vanbellinghen, Nathalie Van houtvin, Sylvain Celanire, Marie-Laure Delporte
Publikováno v:
ChemMedChem. 6:1559-1565
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::d838126cb62c79dcc6d4c0028d307312
https://doi.org/10.1002/cmdc.201100248
https://doi.org/10.1002/cmdc.201100248
Autor:
Frédéric, Denonne, Sylvain, Célanire, Bernard, Christophe, Sabine, Defays, Christel, Delaunoy, Marie-Laure, Delporte, Eric, Detrait, Véronique, Durieu, Michel, Gillard, Yves, Lamberty, Geneviève, Lorent, Jean-Marie, Nicolas, Alain, Vanbellinghen, Nathalie, Van Houtvin, Laurent, Provins
Publikováno v:
ChemMedChem. 6(9)
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::2432afad941b3213430d2db5623a9163
https://pubmed.ncbi.nlm.nih.gov/21761567
https://pubmed.ncbi.nlm.nih.gov/21761567
Autor:
Patrick Pasau, Nathalie Van houtvin, Cecile Pegurier, Thierry Kogej, Frédéric Gilson, Marc Van Thuyne, Sabine Defays, Pierre Danhaive, Michel Gillard, Philippe Collart, BerendJan van Keulen
Publikováno v:
Bioorganicmedicinal chemistry letters. 17(15)
The discovery and optimization of a novel class of potent CCR3 antagonists is described. Details of synthesis and SAR are given together with some ADME properties of selected compounds. An optimal balance between activities, physicochemical propertie
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8e4f740fa3ad5fbadc7d7f3311062490
https://pubmed.ncbi.nlm.nih.gov/17532633
https://pubmed.ncbi.nlm.nih.gov/17532633
Autor:
Alexander Giannaras, Nathalie Van houtvin, Dorin Preda, Dong Zou, Maggi Burton, Frédéric Denonne, Patrick Pasau, Jean-Marie Nicolas, Alan J. Dipesa, Andrew Volosov, Sophie Binet, Philippe Collart, Seema Kumar, Sabine Defays, Maria Eckert, Cecile Pegurier, Beth Levine
Publikováno v:
Bioorganicmedicinal chemistry letters. 17(12)
The synthesis and structure-activity relationships against the C3a receptor of a series of substituted aminopiperidine derivatives are reported. DMPK properties and functional activities of selected compounds are described. The compounds obtained are
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8b3e4b91ef38e5226be91bab95db446a
https://pubmed.ncbi.nlm.nih.gov/17459702
https://pubmed.ncbi.nlm.nih.gov/17459702
Autor:
Laurent Provins, Luc Grooters, Henk Timmerman, Iwan J. P. de Esch, Maikel Wijtmans, Sylvain Celanire, Julien Gérard, Patrice Talaga, Michel Gillard, Frédéric Denonne, Delphine Hubert, Remko A. Bakker, Saskia Hulscher, Sabine Defays, Christel Delaunoy, Rob Leurs, Nathalie Van houtvin
Publikováno v:
MedChemComm, 1, 39-44. Royal Society of Chemistry
Wijtmans, M, Denonne, F, Célanire, S, Gillard, M, Hulscher, T M, Delaunoy, C, Van Houtvin, N, Bakker, R A, Defays, S, Gérard, J, Grooters, L, Hubert, D, Timmerman, H, Leurs, R, Talaga, P, De Esch, I J & Provins, L 2010, ' Histamine H3 receptor ligands with a 3-cyclobutoxy motif: a novel and versatile constraint of the classical 3-propoxy linker ', MedChemComm, vol. 1, pp. 39-44 . https://doi.org/10.1039/c0md00056f
Wijtmans, M, Denonne, F, Célanire, S, Gillard, M, Hulscher, T M, Delaunoy, C, Van Houtvin, N, Bakker, R A, Defays, S, Gérard, J, Grooters, L, Hubert, D, Timmerman, H, Leurs, R, Talaga, P, De Esch, I J & Provins, L 2010, ' Histamine H3 receptor ligands with a 3-cyclobutoxy motif: a novel and versatile constraint of the classical 3-propoxy linker ', MedChemComm, vol. 1, pp. 39-44 . https://doi.org/10.1039/c0md00056f
Antagonists/inverse agonists for the histamine H3 receptor (H3R) are subject to intensive research. Many chemical classes contain a 3-propoxy linker to connect an aromatic moiety and a basic amine. Rigidifying this linker by several moieties has prov
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6990bbedf77cdc518d03fb39d228af03
https://doi.org/10.1039/c0md00056f
https://doi.org/10.1039/c0md00056f