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Bioorg Med Chem Lett. 2013 May 1;23(9):2548-54. doi: 10.1016/j.bmcl.2013.02.118. Epub 2013 Mar 14.

Novel and highly potent histamine H3 receptor ligands. Part 3: an alcohol function to improve the pharmacokinetic profile.

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1
Bioprojet-Biotech, 4 rue du Chesnay Beauregard, BP 96205, 35762 Saint-Grégoire, France. o.labeeuw@bioprojet.com

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.

PMID:
23535326
DOI:
10.1016/j.bmcl.2013.02.118
[Indexed for MEDLINE]
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