三环杂芳族体系1,2,4-三唑并[1,5-a]喹喔啉：合成及苯二氮䓬受体活性
Tricyclic heteroaromatic systems 1,2,4-triazolo[1,5-a]quinoxalines: synthesis and benzodiazepine receptor activity.
作者信息
Catarzi D, Cecchi L, Colotta V, Melani F, Filacchioni G, Martini C, Giusti L, Lucacchini A
机构信息
Dipartimento di Scienze Farmaceutiche, Università di Firenze, Italy.
出版信息
Farmaco. 1993 Aug;48(8):1065-78.
PMID:8216669
Abstract
The synthesis, the benzodiazepine binding activity and the "in vitro" biological effect of some 1,2,4-triazolo[1,5-a]quinoxalines, 3-aza-analogues of some previously reported pyrazolo[1,5-a]quinoxalines, are described. Molecular modelling is used to define the structural requirements of the benzodiazepine recognition site which influence the affinity and different efficacy of these rigid ligands.
摘要
本文描述了一些1,2,4-三唑并[1,5-a]喹喔啉（某些先前报道的吡唑并[1,5-a]喹喔啉的3-氮杂类似物）的合成、苯二氮䓬结合活性及“体外”生物学效应。利用分子建模来确定影响这些刚性配体亲和力和不同效能的苯二氮䓬识别位点的结构要求。
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