N-alkyl-4-[(8-azabicyclo[3.2.1]-oct-3-ylidene)phenylmethyl]benzamides, micro and delta opioid agonists: a micro address.
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.
Carson
John R
JR
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
Coats
Steven J
SJ
Codd
Ellen E
EE
Dax
Scott L
SL
Lee
Jung
J
Martinez
Rebecca P
RP
McKown
Linda A
LA
Anne Neilson
Lou
L
Pitis
Philip M
PM
Wu
Wu-Nan
WN
Zhang
Sui-Po
SP
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
D000700:Analgesics; D001549:Benzamides; D017465:Receptors, Opioid, delta; D017450:Receptors, Opioid, mu