Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1372458 | Bioorganic & Medicinal Chemistry Letters | 2010 | 5 Pages |
Abstract
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.
Graphical abstractThe SAR of a potent series of FLAP inhibitors is described culminating in the identification of lead compound 39 (AM679).Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Nicholas Stock, Christopher Baccei, Gretchen Bain, Alex Broadhead, Charles Chapman, Janice Darlington, Christopher King, Catherine Lee, Yiwei Li, Daniel S. Lorrain, Pat Prodanovich, Haojing Rong, Angelina Santini, Jasmine Zunic, Jilly F. Evans,