Zobrazeno 1 - 5
of 5
pro vyhledávání: '"Olivia Poupardin-Olivier"'
Autor:
Thierry Calmels, Marc Capet, Philippe Robert, Olivier Labeeuw, Denis Danvy, Olivia Poupardin-Olivier, Isabelle Berrebi-Bertrand, C. Robin Ganellin, Walter Schunack, Nicolas Levoin, Holger Stark
Publikováno v:
Archiv der Pharmazie. 341:610-623
Drug-discovery projects frequently employ structure-based information through protein modeling and ligand docking, and there is a plethora of reports relating successful use of them in virtual screening. Hit/lead optimization, which represents the ne
Autor:
Isabelle Berrebi-Bertrand, Olivier Labeeuw, Thierry Calmels, Jean-Charles Schwartz, Olivia Poupardin-Olivier, Marc Capet, Nicolas Levoin, Stéphane Krief, Jeanne-Marie Lecomte
Publikováno v:
Bioorganicmedicinal chemistry. 21(15)
Due to its involvement in major CNS functions, the histamine H3 receptor (H3R) is the subject of intensive medicinal chemistry investigation, supported by the range of modern drug discovery tools, such as receptor modeling and ligand docking. Althoug
Autor:
Marc Capet, Philippe Robert, Thierry Calmels, Jean-Charles Schwartz, Jeanne-Marie Lecomte, Olivia Poupardin-Olivier, Isabelle Berrebi-Bertrand, Olivier Labeeuw, Xavier Ligneau, Nicolas Levoin
Publikováno v:
Bioorganicmedicinal chemistry letters. 23(9)
Synthesis and biological evaluation of potent histamine H3 receptor antagonists incorporating a hydroxyl function are described. Compounds in this series exhibited nanomolar binding affinities for human receptor, illustrating a new possible component
Autor:
Thierry Calmels, Marc Capet, Jean-Charles Schwartz, Olivia Poupardin-Olivier, Nicolas Levoin, Isabelle Berrebi-Bertrand, Jeanne-Marie Lecomte, Olivier Labeeuw
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(18)
Pre-clinical investigation of some aryl-piperidinyl ether histamine H3 receptor antagonists revealed a strong hERG binding. To overcome this issue, we have developed a QSAR model specially dedicated to H3 receptor ligands. This model was designed to
Autor:
Marc Capet, Olivier Labeeuw, Xavier Ligneau, Philippe Robert, Jeanne-Marie Lecomte, Jean-Charles Schwartz, Thierry Calmels, Nicolas Levoin, Olivia Poupardin-Olivier, Isabelle Berrebi-Bertrand
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(18)
Synthesis and biological evaluation of novel and potent cyclohexylamine-based histamine H3 receptor inverse agonists are described. Compounds in this newly identified series exhibited subnanomolar binding affinities for human receptor and no signific