4-Quinolone derivatives: high-affinity ligands at the benzodiazepine site of brain GABAA receptors. Synthesis, pharmacology, and pharmacophore modeling

…, P Andersson, J Nilsson, I Pettersson…

Index: Lager, Erik; Andersson, Pierre; Nilsson, Jakob; Pettersson, Ingrid; Nielsen, Elsebet stergaard; Nielsen, Mogens; Sterner, Olov; Liljefors, Tommy Journal of Medicinal Chemistry, 2006 , vol. 49, # 8 p. 2526 - 2533

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Citation Number: 49

Abstract

The 3-ethoxycarbonyl-4-quinolone compound 1 has previously been identified via a database search as an interesting lead compound for ligand binding at the benzodiazepine site of GABAA receptors (Kahnberg et al. J. Mol. Graphics Modelling 2004, 23, 253-261). Pharmacophore-guided optimization of this lead compound yielded a number of high-affinity ligands for the benzodiazepine site including compounds 20 and 23-25 displaying sub- ...