via-2291 and Coronary-Artery-Disease

5-Lipoxygenase (5-LO)-activating protein (FLAP) inhibitors have proven to attenuate 5-LO pathway activity and leukotriene production in human clinical trials. However, previous clinical candidates have been discontinued and the link between FLAP inhibition and outcome in inflammatory diseases remains to be established. We here describe a novel series of FLAP inhibitors identified from a screen of 10k compounds and the medicinal chemistry strategies undertaken to progress this series. Compound 4i showed good overall properties and a pIC

Topics: 5-Lipoxygenase-Activating Protein Inhibitors; Animals; Caco-2 Cells; Coronary Artery Disease; Cyclohexanes; Dogs; Female; Humans; Leukotriene B4; Male; Molecular Structure; Pyrazoles; Rats, Sprague-Dawley; Structure-Activity Relationship