Novel and highly potent histamine H3 receptor ligands. Part 2: Exploring the cyclohexylamine-based series

DOI: 10.1016/j.bmcl.2011.06.102

Source and publish data:

Bioorganic and Medicinal Chemistry Letters p. 5384 - 5388 (2011)

Update date:2022-08-05

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Authors:

Labeeuw, Olivier

Levoin, Nicolas

Poupardin-Olivier, Olivia

Calmels, Thierry

Ligneau, Xavier

Berrebi-Bertrand, Isabelle

Robert, Philippe

Lecomte, Jeanne-Marie

Schwartz, Jean-Charles

Capet, Marc

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Article abstract of DOI:10.1016/j.bmcl.2011.06.102

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 significant interaction with hERG channel. One derivative (10t) demonstrated enhanced in vivo efficiency and preferential brain distribution, both properties suitable for potential clinical evaluation.

Full text of DOI:10.1016/j.bmcl.2011.06.102

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