2. Academic Validation
  3. Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 6: Opioid receptor binding properties of cyclic variants of 8-carboxamidocyclazocine

Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 6: Opioid receptor binding properties of cyclic variants of 8-carboxamidocyclazocine

  • Bioorg Med Chem. 2008 May 15;16(10):5653-64. doi: 10.1016/j.bmc.2008.03.066.
Mark P Wentland 1,  Xufeng Sun,  Dana J Cohen,  Jean M Bidlack
Affiliations

Affiliation

  • 1 Department of Chemistry and Chemical Biology, Rensselaer Polytechnic Institute, Troy, NY 12180, USA. [email protected]
PMID: 18417347 DOI: 10.1016/j.bmc.2008.03.066
Abstract

A series of 7,8- and 8,9-fused pyrimidinone, aminopyrimidine and pyridone derivatives of 8-carboxamidocyclazocine (8-CAC) have been prepared and evaluated in Opioid Receptor binding assays. Targets were designed to corroborate a pharmacophore hypothesis regarding the bioactive conformation of the carboxamide of 8-CAC. In addition to the results from this study strongly supporting this pharmacophore hypothesis, a number of novel compounds with high affinity to opioid receptors have been identified.

Figures