期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 19, 期 20, 页码 5958-5961出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.08.027
关键词
GABA A; Inverse agonism; Cognitive dysfunction
In a search for GABA(A) alpha 5 ligands that combine high subtype binding selectivity with a marked inverse agonism imidazo[1,5-a][1,2,4]-triazolo[1,5-d][1,4]benzodiazepines were identified as a promising class. A short tandem reaction allowed rapid access to this chemical series, thereby facilitating rapid SAR generation which guided the optimization process. Two compounds (10e and 11f) were found to be active in an in vivo paradigm for cognitive improvement. (C) 2009 Elsevier Ltd. All rights reserved.
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