The synthesis, BZR binding activity, and GABA ratio of some 1,2,4-triazolo[1,5-a]quinoxalines and imidazo[l,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.
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
MARTINI, CLAUDIA;GIUSTI, LAURA;LUCACCHINI, ANTONIO
1994-01-01
Abstract
The synthesis, BZR binding activity, and GABA ratio of some 1,2,4-triazolo[1,5-a]quinoxalines and imidazo[l,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.File in questo prodotto:
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