8-Hydroxyquinolin-2(1H)-one analogues as potential β2-agonists: Design, synthesis and activity study
β2-Agonists that bind to plasmalemmal β2-adrenoceptors causing cAMP accumulation are widely used as bronchodilators in chronic respiratory diseases. Here, we designed and synthesized a group of 8-hydroxyquinolin-2(1H)-one analogues and studied their β2-agonistic activities with a cellular cAMP assay. Compounds B05 and C08 were identified as potent (EC50 2-agonists among the compounds tested. They behaved as partial β2-agonists in non-overexpressed HEK293 cells, and possessed rapid smooth muscle relaxant actions and long duration of action in isolated guinea pig tracheal strip preparations. In summary, B05 and C08 are β2-agonists with potential applicability in chronic respiratory diseases.
Modular Approach to 9-Monosubstituted Fluorene Derivatives Using MoV Reagents
Oxidative coupling using molybdenum(V) reagents provides fast access to highly functionalized 9-monosubstituted fluorenes. This synthetic approach is highly modular, is high yielding, and tolerates a variety of labile moieties, e.g. amides or iodo groups. The established protocol leads to promising precursors for pharmacologically important analogues of melatonin.
Franzmann, Peter,Trosien, Simon,Schubert, Moritz,Waldvogel, Siegfried R.
supporting information
p. 1182 - 1185
(2016/03/15)
Kinetic study of microwave-assisted Wittig reaction of stabilised ylides with aromatic aldehydes
The Wittig reaction of a pool of stabilised ylides and aromatic aldehydes was carried out in a microwave oven. Only a few minutes were needed for high conversion rates under microwave heating in comparison to hour time with traditional methods.
Frattini, Sara,Quai, Monica,Cereda, Enzo
p. 6827 - 6829
(2007/10/03)
More Articles about upstream products of 49621-49-0