Parallel methods for the preparation and SAR exploration of N-ethyl-4-[(8-alkyl-8-aza-bicyclo[3.2.1]oct-3-ylidene)-aryl-methyl]-benzamides, powerful m...
Basic Information
ID: ALA1138013
Journal: Bioorg Med Chem Lett
Title: Parallel methods for the preparation and SAR exploration of N-ethyl-4-[(8-alkyl-8-aza-bicyclo[3.2.1]oct-3-ylidene)-aryl-methyl]-benzamides, powerful mu and delta opioid agonists.
Authors: Coats SJ, Schulz MJ, Carson JR, Codd EE, Hlasta DJ, Pitis PM, Stone DJ, Zhang SP, Colburn RW, Dax SL.
Abstract: Two parallel synthetic methods were developed to explore the structure-activity relationships (SAR) of a series of potent opioid agonists. This series of tropanylidene benzamides proved extremely tolerant of structural variation while maintaining excellent opioid activity. Evaluation of several representative compounds from this series in the mouse hot plate test revealed potent antinociceptive effects upon oral administration.
CiteXplore: 15482911
DOI: 10.1016/j.bmcl.2004.09.004
Patent ID: ┄