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Page 1
Sodium [2'-[(cyclopropanecarbonyl-ethyl-amino)-methyl]-4'-(6-ethoxy-pyridin-3-yl)-6-methoxy-biphenyl-3-yl]-acetate (AM432): a potent, selective prostaglandin D2 receptor antagonist.
Stock N, Volkots D, Stebbins K, Broadhead A, Stearns B, Roppe J, Parr T, Baccei C, Bain G, Chapman C, Correa L, Darlington J, King C, Lee C, Lorrain DS, Prodanovich P, Santini A, Evans JF, Hutchinson JH, Prasit P. Stock N, et al. Among authors: correa l. Bioorg Med Chem Lett. 2011 Feb 1;21(3):1036-40. doi: 10.1016/j.bmcl.2010.12.016. Epub 2010 Dec 9. Bioorg Med Chem Lett. 2011. PMID: 21211969
Pharmacological characterization 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), a novel selective 5-lipoxygenase-activating protein inhibitor that reduces acute and chronic inflammation.
Lorrain DS, Bain G, Correa LD, Chapman C, Broadhead AR, Santini AM, Prodanovich P, Darlington JV, Hutchinson JH, King C, Lee C, Baccei C, Li Y, Arruda JM, Evans JF. Lorrain DS, et al. J Pharmacol Exp Ther. 2009 Dec;331(3):1042-50. doi: 10.1124/jpet.109.158089. Epub 2009 Sep 11. J Pharmacol Exp Ther. 2009. PMID: 19749079
5-Lipoxygenase-activating protein inhibitors. Part 3: 3-{3-tert-Butylsulfanyl-1-[4-(5-methoxy-pyrimidin-2-yl)-benzyl]-5-(5-methyl-pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid (AM643)-A potent FLAP inhibitor suitable for topical administration.
Stock N, Baccei C, Bain G, Chapman C, Correa L, Darlington J, King C, Lee C, Lorrain DS, Prodanovich P, Santini A, Schaab K, Evans JF, Hutchinson JH, Prasit P. Stock N, et al. Among authors: correa l. Bioorg Med Chem Lett. 2010 Aug 1;20(15):4598-601. doi: 10.1016/j.bmcl.2010.06.011. Epub 2010 Jun 8. Bioorg Med Chem Lett. 2010. PMID: 20566292
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. Among authors: correa l. J Med Chem. 2011 Dec 8;54(23):8013-29. doi: 10.1021/jm2008369. Epub 2011 Nov 7. J Med Chem. 2011. PMID: 22059882
Identification of the first potent, selective and bioavailable PPARα antagonist.
Bravo Y, Baccei CS, Broadhead A, Bundey R, Chen A, Clark R, Correa L, Jacintho JD, Lorrain DS, Messmer D, Stebbins K, Prasit P, Stock N. Bravo Y, et al. Among authors: correa l. Bioorg Med Chem Lett. 2014 May 15;24(10):2267-72. doi: 10.1016/j.bmcl.2014.03.090. Epub 2014 Apr 4. Bioorg Med Chem Lett. 2014. PMID: 24745969
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: correa l. 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. Among authors: correa l. J Med Chem. 2009 Oct 8;52(19):5803-15. doi: 10.1021/jm900945d. J Med Chem. 2009. PMID: 19739647
Pharmacology of AM803, a novel selective five-lipoxygenase-activating protein (FLAP) inhibitor in rodent models of acute inflammation.
Lorrain DS, Bain G, Correa LD, Chapman C, Broadhead AR, Santini AM, Prodanovich PP, Darlington JV, Stock NS, Zunic J, King CD, Lee C, Baccei CS, Stearns B, Roppe J, Hutchinson JH, Prasit P, Evans JF. Lorrain DS, et al. Eur J Pharmacol. 2010 Aug 25;640(1-3):211-8. doi: 10.1016/j.ejphar.2010.05.003. Epub 2010 May 21. Eur J Pharmacol. 2010. PMID: 20519143
758 results