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Page 1
Discovery of novel pyrazole-containing benzamides as potent RORγ inverse agonists.
Wang T, Banerjee D, Bohnert T, Chao J, Enyedy I, Fontenot J, Guertin K, Jones H, Lin EY, Marcotte D, Talreja T, Van Vloten K. Wang T, et al. Among authors: guertin k. Bioorg Med Chem Lett. 2015 Aug 1;25(15):2985-90. doi: 10.1016/j.bmcl.2015.05.028. Epub 2015 May 22. Bioorg Med Chem Lett. 2015. PMID: 26048789
Discovery of biaryl carboxylamides as potent RORγ inverse agonists.
Chao J, Enyedy I, Van Vloten K, Marcotte D, Guertin K, Hutchings R, Powell N, Jones H, Bohnert T, Peng CC, Silvian L, Hong VS, Little K, Banerjee D, Peng L, Taveras A, Viney JL, Fontenot J. Chao J, et al. Among authors: guertin k. Bioorg Med Chem Lett. 2015 Aug 1;25(15):2991-7. doi: 10.1016/j.bmcl.2015.05.026. Epub 2015 May 23. Bioorg Med Chem Lett. 2015. PMID: 26048806
Discovery of camphor-derived pyrazolones as 11β-hydroxysteroid dehydrogenase type 1 inhibitors.
Gillespie P, Pietranico-Cole S, Myers M, Bilotta JA, Conde-Knape K, Fotouhi N, Goodnow RA Jr, Guertin KR, Hamilton MM, Haynes NE, Liu B, Qi L, Ren Y, Scott NR, So SS, Spence C, Taub R, Thakkar K, Tilley JW, Zwingelstein C. Gillespie P, et al. Among authors: guertin kr. Bioorg Med Chem Lett. 2014 Jun 15;24(12):2707-11. doi: 10.1016/j.bmcl.2014.04.049. Epub 2014 Apr 21. Bioorg Med Chem Lett. 2014. PMID: 24815509
4-Substituted-7-N-alkyl-N-acetyl 2-aminobenzothiazole amides: drug-like and non-xanthine based A2B adenosine receptor antagonists.
Cheung AW, Brinkman J, Firooznia F, Flohr A, Grimsby J, Gubler ML, Guertin K, Hamid R, Marcopulos N, Norcross RD, Qi L, Ramsey G, Tan J, Wen Y, Sarabu R. Cheung AW, et al. Among authors: guertin k. Bioorg Med Chem Lett. 2010 Jul 15;20(14):4140-6. doi: 10.1016/j.bmcl.2010.05.056. Epub 2010 May 20. Bioorg Med Chem Lett. 2010. PMID: 20541935
Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N-thiazol-2-yl-propionamide (RO0281675).
Haynes NE, Corbett WL, Bizzarro FT, Guertin KR, Hilliard DW, Holland GW, Kester RF, Mahaney PE, Qi L, Spence CL, Tengi J, Dvorozniak MT, Railkar A, Matschinsky FM, Grippo JF, Grimsby J, Sarabu R. Haynes NE, et al. J Med Chem. 2010 May 13;53(9):3618-25. doi: 10.1021/jm100039a. J Med Chem. 2010. PMID: 20405948
Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
Sarabu R, Bizzarro FT, Corbett WL, Dvorozniak MT, Geng W, Grippo JF, Haynes NE, Hutchings S, Garofalo L, Guertin KR, Hilliard DW, Kabat M, Kester RF, Ka W, Liang Z, Mahaney PE, Marcus L, Matschinsky FM, Moore D, Racha J, Radinov R, Ren Y, Qi L, Pignatello M, Spence CL, Steele T, Tengi J, Grimsby J. Sarabu R, et al. J Med Chem. 2012 Aug 23;55(16):7021-36. doi: 10.1021/jm3008689. Epub 2012 Aug 1. J Med Chem. 2012. PMID: 22809456
Identification of a novel class of orally active pyrimido[5,4-3][1,2,4]triazine-5,7-diamine-based hypoglycemic agents with protein tyrosine phosphatase inhibitory activity.
Guertin KR, Setti L, Qi L, Dunsdon RM, Dymock BW, Jones PS, Overton H, Taylor M, Williams G, Sergi JA, Wang K, Peng Y, Renzetti M, Boyce R, Falcioni F, Garippa R, Olivier AR. Guertin KR, et al. Bioorg Med Chem Lett. 2003 Sep 1;13(17):2895-8. doi: 10.1016/s0960-894x(03)00623-1. Bioorg Med Chem Lett. 2003. PMID: 14611852
51 results