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

Abstract：

: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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Labeeuw O,Levoin N,Poupardin-Olivier O,Calmels T,Ligneau X,Berrebi-Bertrand I,Robert P,Lecomte JM,Schwartz JC,Capet M

doi

10.1016/j.bmcl.2011.06.102

subject

Has Abstract

pub_date

2011-09-15 00:00:00

pages

5384-8

issue

18

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(11)00893-6

journal_volume

21

pub_type

杂志文章

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