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
- 1 September 1994
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 37 (18) , 2846-2850
- https://doi.org/10.1021/jm00044a004
Abstract
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.Keywords
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