Structure-Activity Relationships of 1,2,4-Triazolo[1,5-a]quinoxalines and Their 1-Deaza Analogs Imidazo[1,2-a]quinoxalines at the Benzodiazepine Receptor

The synthesis, BZR binding activity, and GABA ratio of some 1,2,4-triazolo[1,5-a]quinoxalines and imidazo[1,2-a]quinoxalines are reported. Both series of compounds displayed similar affinities while their efficacies were different. The structure-activity relationships have provided the opportunity to localize on the BZR accessory areas which are able to enhance the affinity and evaluate the importance of the presence or absence of a proton acceptor atom to determine different trends of efficacy.