Discovery and optimization of novel purines as potent and selective CB2 agonists.

@article{Hollinshead2012DiscoveryAO,
  title={Discovery and optimization of novel purines as potent and selective CB2 agonists.},
  author={Sean P Hollinshead and Peter C Astles and Mark G Chambers and Michael P. Johnson and John Palmer and Michael W. Tidwell},
  journal={Bioorganic & medicinal chemistry letters},
  year={2012},
  volume={22 15},
  pages={4962-6}
}
A focused screening strategy identified thienopyrimidine 1 as a hCB2 cannabinoid receptor agonist with moderate selectivity over the hCB1 receptor. This initial hit suffered from poor in vitro metabolic stability and high in vivo clearance. Structure-activity relationships describe the optimization and modification to a less lipophilic purine core. Examples from this novel series were found to be highly potent and fully efficacious agonists of the human CB2 receptor with excellent selectivity… CONTINUE READING
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References

Publications referenced by this paper.

Compounds which display a high affinity for hERG ion channels are generally considered to have a higher risk of cardiotoxicity Snyders

  • J. D., A. Chaudhary
  • Mol . Pharmacol .
  • 2007

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