24805-59-2Relevant articles and documents
Novel HIV-1 integrase inhibitors derived from quinolone antibiotics
Sato, Motohide,Motomura, Takahisa,Aramaki, Hisateru,Matsuda, Takashi,Yamashita, Masaki,Ito, Yoshiharu,Kawakami, Hiroshi,Matsuzaki, Yuji,Watanabe, Wataru,Yamataka, Kazunobu,Ikeda, Satoru,Kodama, Eiichi,Matsuoka, Masao,Shinkai, Hisashi
, p. 1506 - 1508 (2006)
The viral enzyme integrase is essential for the replication of human immunodeficiency virus type 1 (HIV-1) and represents a remaining target for antiretroviral drugs. Here, we describe the modification of a quinolone antibiotic to produce the novel integr
Use of 2-[18F]fluoroethylazide for the Staudinger ligation - Preparation and characterisation of GABAA receptor binding 4-quinolones
Gaeta, Alessandra,Woodcraft, John,Plant, Stuart,Goggi, Julian,Jones, Paul,Battle, Mark,Trigg, William,Luthra, Sajinder K.,Glaser, Matthias
supporting information; experimental part, p. 4649 - 4652 (2010/10/02)
The labelling reagent 2-[18F]fluoroethylazide was used in a traceless Staudinger ligation. This reaction was employed to obtain the GABAA receptor binding 6-benzyl-4-oxo-1,4-dihydro-quinoline-3- carboxylic acid (2-[18F]flu
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.
