title: 3-(4-Piperidinyl)indoles and 3-(4-piperidinyl)pyrrolo-[2,3-b]pyridines as ligands for the ORL-1 receptor.
abstract: A novel series of indoles and 1H-pyrrolo[2,3-b]pyridines having a piperidine ring at the 3-position were synthesized and found to bind with high affinity to the ORL-1 receptor. Structure-activity relationships at the piperidine nitrogen were investigated in each series. Substitution on the phenyl ring and nitrogen atom of the indole and 1H-pyrrolo[2,3-b]pyridine cores generated several selective high-affinity ligands that were agonists of the ORL-1 receptor.
authors.affiliation: Johnson & Johnson Pharmaceutical Research and Development, L.L.C PO Box 300, 1000 Route 202, Raritan, NJ 08869, USA. gbignan@gmail.com
authors.forename: Gilles C
authors.initials: GC
authors.lastname: Bignan
authors.forename: Kathleen
authors.initials: K
authors.lastname: Battista
authors.forename: Peter J
authors.initials: PJ
authors.lastname: Connolly
authors.forename: Michael J
authors.initials: MJ
authors.lastname: Orsini
authors.forename: Jingchun
authors.initials: J
authors.lastname: Liu
authors.forename: Steven A
authors.initials: SA
authors.lastname: Middleton
authors.forename: Allen B
authors.initials: AB
authors.lastname: Reitz
mesh_terms: D001665:Binding Sites; D007211:Indoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D008024:Ligands; D015394:Molecular Structure; D010880:Piperidines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D011725:Pyridines / Q000737:chemistry / Q000494:pharmacology*; D011758:Pyrroles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D011957:Receptors, Opioid / Q000819:agonists*; D013329:Structure-Activity Relationship; D000094942:Nociceptin Receptor
chemical_list: D007211:Indoles; D008024:Ligands; D010880:Piperidines; D011725:Pyridines; D011758:Pyrroles; D011957:Receptors, Opioid; D000094942:Nociceptin Receptor