132669-28-4Relevant articles and documents
Discovery of N-{1-[3-(3-Oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl] piperidin-4-yl}-2-phenylacetamide (Lu AE51090): An allosteric muscarinic M 1 receptor agonist with unprecedented selectivity and procognitive potential
Sams, Anette G.,Hentzer, Morten,Mikkelsen, Gitte K.,Larsen, Krestian,Bundgaard, Christoffer,Plath, Niels,Christoffersen, Claus T.,Bang-Andersen, Benny
experimental part, p. 6386 - 6397 (2010/11/05)
The discovery and Structure-activity relationship (SAR) of a series of allosteric muscarinic M1 receptor agonists are described. Compound 17 (Lu AE51090) was identified as a representative compound from the series, based on its high selectivity as an agonist at the muscarinic M1 receptor across a panel of muscarinic receptor subtypes. Furthermore, 17 displayed a high degree of selectivity when tested in a broad panel of G-protein-coupled receptors, ion channels, transporters, and enzymes, and 17 showed an acceptable pharmacokinetic profile and sufficient brain exposure in rodents in order to characterize the compound in vivo. Hence, in a rodent model of learning and memory, 17 reversed delay-induced natural forgetting, suggesting a procognitive potential of 17.
Synthesis and biological evaluation of benzo[b]naphthyridones, a series of new topical antibacterial agents
Tabart, Michel,Picaut, Guy,Desconclois, Jean-Francois,Dutka-Malen, Sylvie,Huet, Yvette,Berthaud, Nadine
, p. 919 - 921 (2007/10/03)
We describe here the synthesis and biological evaluation of a series of benzo[b]naphthyridones, a new family of tricyclic antibacterial compounds that have a Gram-positive spectrum of activity. RP60556A, one of the most potent of these compounds, is bactericidal against multiresistant cocci, especially multiresistant Staphylococcus aureus strains. Its physico-chemical and biological properties make it particularly suitable for topical antibacterial use.