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Discovery of potent and selective PPARα/δ dual antagonists and initial biological studies.
Jacintho JD, Baccei CS, Bravo Y, Broadhead A, Chen A, Correa L, Fischer K, Laffitte B, Lee C, Lorrain DS, Messmer D, Prasit P, Stebbins KJ, Stock NS. Jacintho JD, et al. Among authors: lorrain ds. Bioorg Med Chem Lett. 2019 Feb 1;29(3):503-508. doi: 10.1016/j.bmcl.2018.12.045. Epub 2018 Dec 21. Bioorg Med Chem Lett. 2019. PMID: 30594433
5-lipoxygenase-activating protein inhibitors: development of 3-[3-tert-butylsulfanyl-1-[4-(6-methoxy-pyridin-3-yl)-benzyl]-5-(pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid (AM103).
Hutchinson JH, Li Y, Arruda JM, Baccei C, Bain G, Chapman C, Correa L, Darlington J, King CD, Lee C, Lorrain D, Prodanovich P, Rong H, Santini A, Stock N, Prasit P, Evans JF. Hutchinson JH, et al. J Med Chem. 2009 Oct 8;52(19):5803-15. doi: 10.1021/jm900945d. J Med Chem. 2009. PMID: 19739647
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.
Stock NS, Bain G, Zunic J, Li Y, Ziff J, Roppe J, Santini A, Darlington J, Prodanovich P, King CD, Baccei C, Lee C, Rong H, Chapman C, Broadhead A, Lorrain D, Correa L, Hutchinson JH, Evans JF, Prasit P. Stock NS, et al. J Med Chem. 2011 Dec 8;54(23):8013-29. doi: 10.1021/jm2008369. Epub 2011 Nov 7. J Med Chem. 2011. PMID: 22059882
60 results