64321-60-4Relevant academic research and scientific papers
Investigations on the 4-quinolone-3-carboxylic acid motif. 2. Synthesis and structure-activity relationship of potent and selective cannabinoid-2 receptor agonists endowed with analgesic activity in vivo
Pasquini, Serena,Botta, Lorenzo,Semeraro, Teresa,Mugnaini, Claudia,Ligresti, Alessia,Palazzo, Enza,Maione, Sabatino,Di Marzo, Vincenzo,Corelli, Federico
supporting information; experimental part, p. 5075 - 5084 (2009/07/25)
Quinolone-3-carboxamides 11 bearing at position 5, 6, 7, or 8 diverse substituents such as halides, alkyl, aryl, alkoxy, and aryloxy groups differing in their steric/electronic properties, were prepared. The new compounds were tested in vitro for CB1 and
4-Quinolone derivatives: High-affinity ligands at the benzodiazepine site of brain GABAA receptors. Synthesis, pharmacology, and pharmacophore modeling
Lager, Erik,Andersson, Pierre,Nilsson, Jakob,Pettersson, Ingrid,Nielsen, Elsebet ?stergaard,Nielsen, Mogens,Sterner, Olov,Liljefors, Tommy
, p. 2526 - 2533 (2007/10/03)
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-nanomolar affinities. A few of the compounds have been tested on the α1β 2γ2S and α3β 2γ2S GABAA receptor subtypes, and two of the compounds (5 and 19) display selectivity for α1-versus α3-containing receptors by a factor of 22 and 27, respectively. This selectivity for α1β2γ2S is in the same range as that for the well-known α1 subunit selective compound zolpidem.
