Fluorinated non-imidazole histamine H3 receptor antagonists

Fluorine substituents have become a widespread and important component in drug design and development. Here, the synthesis of fluorine containing compounds and some corresponding precursor molecules are presented for potential isotope labelling as well as their data obtained with in vitro and in viv...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2009-04, Vol.19 (8), p.2172-2175
Main Authors: ISENSEE, K, AMON, M, GALAPARTI, A, LIGNEAU, X, CAMELIN, J.-C, CAPET, M, SCHWARTZ, J.-C, STARK, H
Format: Article
Language:English
Subjects:
Animals
Biological and medical sciences
Fluorine - chemistry
Fluorine - metabolism
Fluorine - pharmacology
Histamine H3 Antagonists - chemistry
Histamine H3 Antagonists - metabolism
Histamine H3 Antagonists - pharmacology
Imidazoles - chemistry
Imidazoles - pharmacology
Medical sciences
Mice
Miscellaneous
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Pharmacology. Drug treatments
Protein Binding - drug effects
Receptors, Histamine H3 - chemistry
Receptors, Histamine H3 - metabolism
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Summary:Fluorine substituents have become a widespread and important component in drug design and development. Here, the synthesis of fluorine containing compounds and some corresponding precursor molecules are presented for potential isotope labelling as well as their data obtained with in vitro and in vivo screenings. The compounds vary in the basic centres (piperidine or pyrrolidine) and are fluoro substituted in different positions of the basic alicyclic moiety. Pharmacological evaluation resulted in ligands with high affinities at hH(3) receptor in the nanomolar and subnanomolar concentration range and some with high antagonist in vivo potencies.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2009.02.110