Discovery of a series of aryl-N-(3-(alkylamino)-5-(trifluoromethyl)phenyl)benzamides as TRPA1 antagonists

We describe the discovery and advancement of a novel series of TRPA1 antagonist having an aryl-N-(3-(alkylamino)-5-(trifluoromethyl)phenyl)benzamide scaffold. The physical and in vitro DMPK profiles are discussed.

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2014-07, Vol.24 (14), p.3204-3206
Main Authors: Laliberté, Sébastien, Vallée, Frédéric, Fournier, Pierre-André, Bedard, Leanne, Labrecque, Jean, Albert, Jeffrey S.
Format: Article
Language:English
Subjects:
Antagonist
Benzamides - chemical synthesis
Benzamides - chemistry
Benzamides - pharmacology
Calcium Channels
Dose-Response Relationship, Drug
Drug Discovery
Humans
Ligand gated ion channel
Molecular Structure
Nerve Tissue Proteins - antagonists & inhibitors
Structure-Activity Relationship
Transient Receptor Potential Channels - antagonists & inhibitors
TRPA1
TRPA1 Cation Channel
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Description
Summary:We describe the discovery and advancement of a novel series of TRPA1 antagonist having an aryl-N-(3-(alkylamino)-5-(trifluoromethyl)phenyl)benzamide scaffold. The physical and in vitro DMPK profiles are discussed.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2014.05.013