title: N-alkyl-4-[(8-azabicyclo[3.2.1]-oct-3-ylidene)phenylmethyl]benzamides, micro and delta opioid agonists: a micro address.
abstract: The tertiary amide delta opioid agonist 2 is a potent antinociceptive agent. Compound 2 was metabolized in vitro and in vivo to secondary amide 3, a potent and selective micro opioid agonist. The SAR of a series of N-alkyl-4-[(8-azabicyclo[3.2.1]-oct-3-ylidene)phenylmethyl]benzamides was examined.
authors.affiliation: Drug Discovery, Johnson and Johnson Pharmaceutical Research and Development, LLC, Welsh and McKean Roads, PO 776, Spring House, PA 19477-0776, USA. jcarson@prdus.jnj.edu
authors.forename: John R
authors.initials: JR
authors.lastname: Carson
authors.forename: Steven J
authors.initials: SJ
authors.lastname: Coats
authors.forename: Ellen E
authors.initials: EE
authors.lastname: Codd
authors.forename: Scott L
authors.initials: SL
authors.lastname: Dax
authors.forename: Jung
authors.initials: J
authors.lastname: Lee
authors.forename: Rebecca P
authors.initials: RP
authors.lastname: Martinez
authors.forename: Linda A
authors.initials: LA
authors.lastname: McKown
authors.forename: Lou
authors.initials: L
authors.lastname: Anne Neilson
authors.forename: Philip M
authors.initials: PM
authors.lastname: Pitis
authors.forename: Wu-Nan
authors.initials: WN
authors.lastname: Wu
authors.forename: Sui-Po
authors.initials: SP
authors.lastname: Zhang
mesh_terms: D000700:Analgesics / Q000737:chemistry / Q000494:pharmacology*; D001549:Benzamides / Q000737:chemistry / Q000494:pharmacology*; D017465:Receptors, Opioid, delta / Q000819:agonists*; D017450:Receptors, Opioid, mu / Q000819:agonists*; D013329:Structure-Activity Relationship
chemical_list: D000700:Analgesics; D001549:Benzamides; D017465:Receptors, Opioid, delta; D017450:Receptors, Opioid, mu