Cinnamic amides of (S)-2-(aminomethyl)pyrrolidines are potent H3 antagonists

New imidazole-free H3 antagonists have been found in a series of cinnamic amides of (S)-(aminomethyl)pyrrolidines. The influence of the substituent on the aromatic moiety on the potency and the inhibition of three cytochrome P450 subtypes are also described.

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry 2004-05, Vol.12 (10), p.2603-2616
Main Authors: PESCHKE, Bernd, BAK, Sonja, HOHLWEG, Rolf, PETTERSSON, Ingrid, HOFFMANN FRØLUND REFSGAARD, Hanne, VIUFF, Dorthe, RIMVALL, Karin
Format: Article
Language:English
Subjects:
Amides - chemistry
Amides - pharmacology
Animals
Biological and medical sciences
CHO Cells
Cinnamates - chemistry
Cinnamates - pharmacology
Cricetinae
Cricetulus
Cytochrome P-450 Enzyme Inhibitors
Guanosine 5'-O-(3-Thiotriphosphate) - metabolism
Histamine Antagonists - chemical synthesis
Histamine Antagonists - chemistry
Histamine Antagonists - pharmacology
Medical sciences
Miscellaneous
Molecular Structure
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Pharmacology. Drug treatments
Pyrrolidines - chemistry
Pyrrolidines - pharmacology
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Description
Summary:New imidazole-free H3 antagonists have been found in a series of cinnamic amides of (S)-(aminomethyl)pyrrolidines. The influence of the substituent on the aromatic moiety on the potency and the inhibition of three cytochrome P450 subtypes are also described.
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2004.03.021