| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 10591903 | Bioorganic & Medicinal Chemistry Letters | 2013 | 7 Pages |
Abstract
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 for the H3 pharmacophore. As demonstrated with compound BP1.4160 (cyclohexanol 19), the introduction of an alcohol function counter-intuitively allowed to reach high in vivo efficiency and favorable pharmacokinetic profile with reduced half-life.
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Authors
Olivier Labeeuw, Nicolas Levoin, Olivia Poupardin-Olivier, Thierry Calmels, Xavier Ligneau, Isabelle Berrebi-Bertrand, Philippe Robert, Jeanne-Marie Lecomte, Jean-Charles Schwartz, Marc Capet,