N-alkyl-4-[(8-azabicyclo[3.2.1]-oct-3-ylidene)phenylmethyl]benzamides, micro and delta opioid agonists: a micro address

John R Carson; Steven J Coats; Ellen E Codd; Scott L Dax; Jung Lee; Rebecca P Martinez; Linda A McKown; Lou Anne Neilson; Philip M Pitis; Wu-Nan Wu; Sui-Po Zhang

doi:10.1016/j.bmcl.2004.02.052

N-alkyl-4-[(8-azabicyclo[3.2.1]-oct-3-ylidene)phenylmethyl]benzamides, micro and delta opioid agonists: a micro address

Bioorg Med Chem Lett. 2004 May 3;14(9):2113-6. doi: 10.1016/j.bmcl.2004.02.052.

Authors

John R Carson¹, Steven J Coats, Ellen E Codd, Scott L Dax, Jung Lee, Rebecca P Martinez, Linda A McKown, Lou Anne Neilson, Philip M Pitis, Wu-Nan Wu, Sui-Po Zhang

Affiliation

¹ Drug Discovery, Johnson and Johnson Pharmaceutical Research and Development, LLC, Welsh and McKean Roads, PO 776, Spring House, PA 19477-0776, USA. [email protected]

PMID: 15080990
DOI: 10.1016/j.bmcl.2004.02.052

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.

MeSH terms

Analgesics / chemistry
Analgesics / pharmacology*
Benzamides / chemistry
Benzamides / pharmacology*
Receptors, Opioid, delta / agonists*
Receptors, Opioid, mu / agonists*
Structure-Activity Relationship

Substances

Analgesics
Benzamides
Receptors, Opioid, delta
Receptors, Opioid, mu