title: Synthesis and structure-activity relationships of a new series of 2alpha-substituted trans-4,5-dimethyl-4-(3-hydroxyphenyl)piperidine as mu-selective opioid antagonists.
abstract: Structure-activity relationships at the 2alpha-position of the piperidine ring of the trans-4,5-dimethyl-4-(3-hydroxyphenyl)piperidine mu-opioid antagonist series were investigated. This study showed that only small linear alkyl groups (methyl, propyl) are tolerated at the 2alpha-position of the piperidine ring of this series.
authors.affiliation: Department of Chemistry, Adolor Corporation, 700 Pennsylvania Drive, Exton, PA 19341, USA. blebourdonnec@adolor.com
authors.forename: Bertrand
authors.initials: B
authors.lastname: Le Bourdonnec
authors.forename: Allan J
authors.initials: AJ
authors.lastname: Goodman
authors.forename: Mathieu
authors.initials: M
authors.lastname: Michaut
authors.forename: Hai-Fen
authors.initials: HF
authors.lastname: Ye
authors.forename: Thomas M
authors.initials: TM
authors.lastname: Graczyk
authors.forename: Serge
authors.initials: S
authors.lastname: Belanger
authors.forename: Robert N
authors.initials: RN
authors.lastname: DeHaven
authors.forename: Roland E
authors.initials: RE
authors.lastname: Dolle
mesh_terms: D018360:Crystallography, X-Ray; D008958:Models, Molecular; D008968:Molecular Conformation; D010880:Piperidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D017450:Receptors, Opioid, mu / Q000037:antagonists & inhibitors*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D010880:Piperidines; D017450:Receptors, Opioid, mu