Catarzi D, Cecchi L, Colotta V, Melani F, Filacchioni G, Martini C, Giusti L, Lucacchini A
Dipartimento di Scienze Farmaceutiche, Università di Firenze, Italy.
J Med Chem. 1994 Sep 2;37(18):2846-50. doi: 10.1021/jm00044a004.
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.
报道了一些1,2,4-三唑并[1,5-a]喹喔啉和咪唑并[1,2-a]喹喔啉的合成、苯二氮卓受体（BZR）结合活性及γ-氨基丁酸（GABA）比率。这两类化合物表现出相似的亲和力，但其效力不同。构效关系为定位能够增强亲和力的BZR辅助区域提供了机会，并评估了质子受体原子的存在与否对确定不同效力趋势的重要性。
