Benzo[7]annulene-based GluN2B selective NMDA receptor antagonists: Surprising effect of a nitro group in 2-position.

@article{Gawaskar2015Benzo7annulenebasedGS,
  title={Benzo[7]annulene-based GluN2B selective NMDA receptor antagonists: Surprising effect of a nitro group in 2-position.},
  author={Sandeep Gawaskar and Dirk Schepmann and Alessandro Bonifazi and Dina Robaa and Wolfgang Sippl and Bernhard W{\"u}nsch},
  journal={Bioorganic & medicinal chemistry letters},
  year={2015},
  volume={25 24},
  pages={5748-51}
}
Benzo[7]annulen-7-amines 7 without further polar substituents have been reported as conformationally restricted Ro 25-6981 analogs and show unexpectedly high GluN2B affinity. Herein the corresponding 2-NO2 derivatives 8 were synthesized and pharmacologically evaluated. NO2 derivatives 8 show 5- to 10-fold higher GluN2B affinity than the unsubstituted… CONTINUE READING