Benzimidazolone bioisosteres of potent GluN2B selective NMDA receptor antagonists

Bioisosteric replacement of the phenol of potent GluN2B antagonists led to [7]annulenobenzimidazonoes. Intermediate tricyclic alcohol was prepared in a seven-step synthesis. Five additional steps provided phenylpropylamine showing moderate GluN2B affinity.91