950701-46-9Relevant academic research and scientific papers
5-Lipoxygenase-activating protein inhibitors. Part 2: 3-{5-((S)-1-Acetyl-2,3-dihydro-1H-indol-2-ylmethoxy)-3-tert-butylsulfanyl-1-[4-(5-methoxy-pyrimidin-2-yl)-benzyl]-1H-indol-2-yl}-2,2-dimethyl-propionic acid (AM679)-A potent FLAP inhibitor
Stock, Nicholas,Baccei, Christopher,Bain, Gretchen,Broadhead, Alex,Chapman, Charles,Darlington, Janice,King, Christopher,Lee, Catherine,Li, Yiwei,Lorrain, Daniel S.,Prodanovich, Pat,Rong, Haojing,Santini, Angelina,Zunic, Jasmine,Evans, Jilly F.,Hutchinson, John H.,Prasit, Peppi
scheme or table, p. 213 - 217 (2010/04/24)
A series of potent 5-lipoxygenase-activating protein (FLAP) inhibitors are herein described. SAR studies focused on the discovery of novel alicyclic moieties appended to an indole core to optimize potency, physical properties and off-target activities. Subsequent SAR on the N-benzyl substituent of the indole led to the discovery of compound 39 (AM679) which showed potent inhibition of leukotrienes in human blood and in a rodent bronchoalvelolar lavage (BAL) challenge model.
