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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: chen a. 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
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: chen a. 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
A Selective Novel Peroxisome Proliferator-Activated Receptor (PPAR)-α Antagonist Induces Apoptosis and Inhibits Proliferation of CLL Cells In Vitro and In Vivo.
Messmer D, Lorrain K, Stebbins K, Bravo Y, Stock N, Cabrera G, Correa L, Chen A, Jacintho J, Chiorazzi N, Yan XJ, Spaner D, Prasit P, Lorrain D. Messmer D, et al. Among authors: chen a. Mol Med. 2015 Jun 9;21(1):410-9. doi: 10.2119/molmed.2015.00139. Mol Med. 2015. PMID: 26070013 Free PMC article.
The discovery and synthesis of potent zwitterionic inhibitors of renin.
Aspiotis R, Chen A, Cauchon E, Dubé D, Falgueyret JP, Gagné S, Gallant M, Grimm EL, Houle R, Juteau H, Lacombe P, Laliberté S, Lévesque JF, MacDonald D, McKay D, Percival MD, Roy P, Soisson SM, Wu T. Aspiotis R, et al. Among authors: chen a. Bioorg Med Chem Lett. 2011 Apr 15;21(8):2430-6. doi: 10.1016/j.bmcl.2011.02.067. Epub 2011 Feb 18. Bioorg Med Chem Lett. 2011. PMID: 21429746
Renin inhibitors for the treatment of hypertension: design and optimization of a novel series of pyridone-substituted piperidines.
Chen A, Campeau LC, Cauchon E, Chefson A, Ducharme Y, Dubé D, Falgueyret JP, Fournier PA, Gagné S, Grimm E, Han Y, Houle R, Huang JQ, Lacombe P, Laliberté S, Lévesque JF, Liu S, MacDonald D, Mackay B, McKay D, Percival MD, Regan C, Regan H, St-Jacques R, Toulmond S. Chen A, et al. Bioorg Med Chem Lett. 2011 Jul 1;21(13):3970-5. doi: 10.1016/j.bmcl.2011.05.013. Epub 2011 May 14. Bioorg Med Chem Lett. 2011. PMID: 21621998
3,4-Diarylpiperidines as potent renin inhibitors.
Lacombe P, Arbour M, Aspiotis R, Cauchon E, Chen A, Dubé D, Falgueyret JP, Fournier PA, Gallant M, Grimm E, Han Y, Juteau H, Liu S, Mellon C, Ramtohul Y, Simard D, St-Jacques R, Tsui GC. Lacombe P, et al. Among authors: chen a. Bioorg Med Chem Lett. 2012 Mar 1;22(5):1953-7. doi: 10.1016/j.bmcl.2012.01.044. Epub 2012 Jan 26. Bioorg Med Chem Lett. 2012. PMID: 22325946
Identification of a new biaryl scaffold generating potent renin inhibitors.
Lacombe P, Aspiotis R, Bayly C, Chen A, Dubé D, Fortin R, Gallant M, Juteau H, Liu S, McKay D, Roy P, Wu T. Lacombe P, et al. Among authors: chen a. Bioorg Med Chem Lett. 2010 Oct 1;20(19):5822-6. doi: 10.1016/j.bmcl.2010.07.127. Epub 2010 Aug 3. Bioorg Med Chem Lett. 2010. PMID: 20728350
Design and synthesis of potent, isoxazole-containing renin inhibitors.
Fournier PA, Arbour M, Cauchon E, Chen A, Chefson A, Ducharme Y, Falgueyret JP, Gagné S, Grimm E, Han Y, Houle R, Lacombe P, Lévesque JF, MacDonald D, Mackay B, McKay D, Percival MD, Ramtohul Y, St-Jacques R, Toulmond S. Fournier PA, et al. Among authors: chen a. Bioorg Med Chem Lett. 2012 Apr 15;22(8):2670-4. doi: 10.1016/j.bmcl.2012.03.014. Epub 2012 Mar 11. Bioorg Med Chem Lett. 2012. PMID: 22450130
Impact of passive permeability and gut efflux transport on the oral bioavailability of novel series of piperidine-based renin inhibitors in rodents.
Lévesque JF, Bleasby K, Chefson A, Chen A, Dubé D, Ducharme Y, Fournier PA, Gagné S, Gallant M, Grimm E, Hafey M, Han Y, Houle R, Lacombe P, Laliberté S, MacDonald D, Mackay B, Papp R, Tschirret-Guth R. Lévesque JF, et al. Among authors: chen a. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5547-51. doi: 10.1016/j.bmcl.2011.06.095. Epub 2011 Jun 28. Bioorg Med Chem Lett. 2011. PMID: 21784634
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