title: Discovery of a series of aryl-N-(3-(alkylamino)-5-(trifluoromethyl)phenyl)benzamides as TRPA1 antagonists.
abstract: 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.
authors.affiliation: AstraZeneca/OmegaChem, Department of Medicinal Chemistry, Montréal H4S 1Z9, Canada.
authors.forename: Sébastien
authors.initials: S
authors.lastname: Laliberté
authors.affiliation: AstraZeneca/OmegaChem, Department of Medicinal Chemistry, Montréal H4S 1Z9, Canada.
authors.forename: Frédéric
authors.initials: F
authors.lastname: Vallée
authors.affiliation: AstraZeneca/OmegaChem, Department of Medicinal Chemistry, Montréal H4S 1Z9, Canada.
authors.forename: Pierre-André
authors.initials: PA
authors.lastname: Fournier
authors.affiliation: AstraZeneca, DMPK, Montréal H4S 1Z9, Canada.
authors.forename: Leanne
authors.initials: L
authors.lastname: Bedard
authors.affiliation: AstraZeneca, Department of Bioscience, Montréal H4S 1Z9, Canada.
authors.forename: Jean
authors.initials: J
authors.lastname: Labrecque
authors.affiliation: AstraZeneca, Department of Chemistry, Montréal H4S 1Z9, Canada. Electronic address: Jeffrey.Albert@IntelliSynRD.com.
authors.forename: Jeffrey S
authors.initials: JS
authors.lastname: Albert
mesh_terms: D001549:Benzamides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D015220:Calcium Channels; D004305:Dose-Response Relationship, Drug; D055808:Drug Discovery; D006801:Humans; D015394:Molecular Structure; D009419:Nerve Tissue Proteins / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D000074025:TRPA1 Cation Channel; D050051:Transient Receptor Potential Channels / Q000037:antagonists & inhibitors*
chemical_list: D001549:Benzamides; D015220:Calcium Channels; D009419:Nerve Tissue Proteins; D000074025:TRPA1 Cation Channel; C473350:TRPA1 protein, human; D050051:Transient Receptor Potential Channels
keywords: Antagonist; Ligand gated ion channel; TRPA1