8-Substituted 1,3-dimethyltetrahydropyrazino[2,1-f]purinediones: Water-soluble adenosine receptor antagonists and monoamine oxidase B inhibitors

Autor: Andreas Brunschweiger, Jörg Hockemeyer, Frédéric Denonne, Muhammad Rafehi, Michael Wiese, Jag Paul Heer, Pierre Koch, Miriam Schlenk, Sonja Hinz, H. Radjainia, Christa E. Müller, Petra Küppers, Felipe Pineda

Publikováno v: Bioorganicmedicinal chemistry. 24(21)

Multitarget approaches, i.e., addressing two or more targets simultaneously with a therapeutic agent, are hypothesized to offer additive therapeutic benefit for the treatment of neurodegenerative diseases. Validated targets for the treatment of Parki

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dd8b794bbca4ab67d1650da434424664
https://pubmed.ncbi.nlm.nih.gov/27658798

Acetamide Scanning around Bicyclic Thiazoles: SAR at the H3 Receptor

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

Discovery of a New Class of Non-imidazole Oxazoline-Based Histamine H3Receptor (H3R) Inverse Agonists

Autor: Iwan J. P. de Esch, Yves Lamberty, Patrice Talaga, Valérie Verbois, Rob Leurs, Frédéric Denonne, Florence Lebon, Alain Vanbellinghen, Bernard Christophe, Michel Gillard, Christel Delaunoy, Sylvain Celanire, Edith Gelens, Erwin Snip, Henk Timmerman, Donald Dassesse, Nathalie Van houtvin, Laurent Provins, Benedicte Lallemand, Véronique Durieu, Philippe Collart, Jean-Marie Nicolas, Maikel Wijtmans, Luc Quere

Publikováno v: ChemMedChem, 4(7), 1063-8. John Wiley and Sons Ltd
Celanire, S, Wijtmans, M, Christophe, B, Collart, P, de Esch, I J P, Dassesse, D, Delaunoy, C, Denonne, F, Durieu, V, Gelens, E, Gillard, M, Lallemand, B, Lamberty, Y, Lebon, F, Nicolas, J M, Quere, L, Snip, E, Vanbellinghen, A, Van Houtvin, N, Verbois, V, Timmerman, H, Talaga, P, Leurs, R & Provins, L 2009, ' Discovery of a new class of non-imidazole oxazoline-based histamine H(3) receptor (H(3)R) inverse agonists ', ChemMedChem, vol. 4, no. 7, pp. 1063-8 . https://doi.org/10.1002/cmdc.200900055

H(3)R inverse agonists based on an aminopropoxy-phenyloxazoline framework constitute highly valuable druglike lead compounds that display efficacy in a mouse model of recognition memory.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::543d6a72ee98e4081c29c96d0b654379
https://doi.org/10.1002/cmdc.200900055

Discovery of new C3aR ligands. Part 2: amino-piperidine derivatives

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

Histamine H3 receptor ligands with a 3-cyclobutoxy motif: a novel and versatile constraint of the classical 3-propoxy linker

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

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