5-Lipoxygenase-activating protein (FLAP) inhibitors. Part 4: development of 3-[3-tert-butylsulfanyl-1-[4-(6-ethoxypyridin-3-yl)benzyl]-5-(5-methylpyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethylpropionic acid (AM803), a potent, oral, once daily FLAP inhibitor.

@article{Stock20115LipoxygenaseactivatingP,
  title={5-Lipoxygenase-activating protein (FLAP) inhibitors. Part 4: development of 3-[3-tert-butylsulfanyl-1-[4-(6-ethoxypyridin-3-yl)benzyl]-5-(5-methylpyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethylpropionic acid (AM803), a potent, oral, once daily FLAP inhibitor.},
  author={Nicholas Simon Stock and Gretchen Bain and J Marija Zunic and Yiwei Li and Jeannie Ziff and Jeffrey Roger Roppe and Angelina M. Santini and Janice V Darlington and Pat Prodanovich and Christopher D. King and Christopher S. Baccei and Catherine A. A. Lee and Haojing Rong and Charles Patrick Chapman and Alex R. Broadhead and Dan Lorrain and Lucia D. Correa and John H Hutchinson and Jeffrey S. Evans and Peppi Prasit},
  journal={Journal of medicinal chemistry},
  year={2011},
  volume={54 23},
  pages={
          8013-29
        }
}
The potent 5-lipoxygenase-activating protein (FLAP) inhibitor 3-[3-tert-butylsulfanyl-1-[4-(6-ethoxypyridin-3-yl)benzyl]-5-(5-methylpyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethylpropionic acid 11cc is described (AM803, now GSK2190915). Building upon AM103 (1) (Hutchinson et al. J. Med Chem.2009, 52, 5803-5815; Stock et al. Bioorg. Med. Chem. Lett. 2010, 20, 213-217; Stock et al. Bioorg. Med. Chem. Lett.2010, 20, 4598-4601), SAR studies centering around the pyridine moiety led to the discovery… CONTINUE READING
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