Affinity of 3-acyl substituted 4-quinolones at the benzodiazepine site of GABA A receptors

…, J Nilsson, EØ Nielsen, M Nielsen, T Liljefors…

Index: Lager, Erik; Nilsson, Jakob; stergaard Nielsen, Elsebet; Nielsen, Mogens; Liljefors, Tommy; Sterner, Olov Bioorganic and Medicinal Chemistry, 2008 , vol. 16, # 14 p. 6936 - 6948

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Citation Number: 11

Abstract

The finding that alkyl 1, 4-dihydro-4-oxoquinoline-3-carboxylate and N-alkyl-1, 4-dihydro-4- oxoquinoline-3-carboxamide derivatives may be high-affinity ligands at the benzodiazepine binding site of the GABAA receptor, prompted a study of 3-acyl-1, 4-dihydro-4-oxoquinoline (3-acyl-4-quinolones). In general, the affinity of the 3-acyl derivatives was found to be comparable with the 3-carboxylate and the 3-carboxamide derivatives, and certain ...