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Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus.
Pfefferkorn JA, Guzman-Perez A, Litchfield J, Aiello R, Treadway JL, Pettersen J, Minich ML, Filipski KJ, Jones CS, Tu M, Aspnes G, Risley H, Bian J, Stevens BD, Bourassa P, D'Aquila T, Baker L, Barucci N, Robertson AS, Bourbonais F, Derksen DR, Macdougall M, Cabrera O, Chen J, Lapworth AL, Landro JA, Zavadoski WJ, Atkinson K, Haddish-Berhane N, Tan B, Yao L, Kosa RE, Varma MV, Feng B, Duignan DB, El-Kattan A, Murdande S, Liu S, Ammirati M, Knafels J, Dasilva-Jardine P, Sweet L, Liras S, Rolph TP. Pfefferkorn JA, et al. Among authors: macdougall m. J Med Chem. 2012 Feb 9;55(3):1318-33. doi: 10.1021/jm2014887. Epub 2012 Jan 24. J Med Chem. 2012. PMID: 22196621
The design and synthesis of indazole and pyrazolopyridine based glucokinase activators for the treatment of type 2 diabetes mellitus.
Pfefferkorn JA, Tu M, Filipski KJ, Guzman-Perez A, Bian J, Aspnes GE, Sammons MF, Song W, Li JC, Jones CS, Patel L, Rasmusson T, Zeng D, Karki K, Hamilton M, Hank R, Atkinson K, Litchfield J, Aiello R, Baker L, Barucci N, Bourassa P, Bourbonais F, D'Aquila T, Derksen DR, MacDougall M, Robertson A. Pfefferkorn JA, et al. Among authors: macdougall m. Bioorg Med Chem Lett. 2012 Dec 1;22(23):7100-5. doi: 10.1016/j.bmcl.2012.09.082. Epub 2012 Sep 29. Bioorg Med Chem Lett. 2012. PMID: 23089526
Discovery of an intravenous hepatoselective glucokinase activator for the treatment of inpatient hyperglycemia.
Stevens BD, Litchfield J, Pfefferkorn JA, Atkinson K, Perreault C, Amor P, Bahnck K, Berliner MA, Calloway J, Carlo A, Derksen DR, Filipski KJ, Gumkowski M, Jassal C, MacDougall M, Murphy B, Nkansah P, Pettersen J, Rotter C, Zhang Y. Stevens BD, et al. Among authors: macdougall m. Bioorg Med Chem Lett. 2013 Dec 15;23(24):6588-92. doi: 10.1016/j.bmcl.2013.10.057. Epub 2013 Nov 4. Bioorg Med Chem Lett. 2013. PMID: 24239482
PDE-10A inhibitors as insulin secretagogues.
Cantin LD, Magnuson S, Gunn D, Barucci N, Breuhaus M, Bullock WH, Burke J, Claus TH, Daly M, Decarr L, Gore-Willse A, Hoover-Litty H, Kumarasinghe ES, Li Y, Liang SX, Livingston JN, Lowinger T, Macdougall M, Ogutu HO, Olague A, Ott-Morgan R, Schoenleber RW, Tersteegen A, Wickens P, Zhang Z, Zhu J, Zhu L, Sweet LJ. Cantin LD, et al. Among authors: macdougall m. Bioorg Med Chem Lett. 2007 May 15;17(10):2869-73. doi: 10.1016/j.bmcl.2007.02.061. Epub 2007 Feb 25. Bioorg Med Chem Lett. 2007. PMID: 17400452
Optimization of the 4-aryl group of 4-aryl-pyridine glucagon antagonists: development of an efficient, alternative synthesis.
Smith RA, Hertzog DL, Osterhout MH, Ladouceur GH, Korpusik M, Bobko MA, Jones JH, Phelan K, Romero RH, Hundertmark T, MacDougall ML, Livingston JN, Schoen WR. Smith RA, et al. Among authors: macdougall ml. Bioorg Med Chem Lett. 2002 May 6;12(9):1303-6. doi: 10.1016/s0960-894x(02)00143-9. Bioorg Med Chem Lett. 2002. PMID: 11965376
Integration of optimized substituent patterns to produce highly potent 4-aryl-pyridine glucagon receptor antagonists.
Ladouceur GH, Cook JH, Hertzog DL, Jones JH, Hundertmark T, Korpusik M, Lease TG, Livingston JN, MacDougall ML, Osterhout MH, Phelan K, Romero RH, Schoen WR, Shao C, Smith RA. Ladouceur GH, et al. Among authors: macdougall ml. Bioorg Med Chem Lett. 2002 Dec 2;12(23):3421-4. doi: 10.1016/s0960-894x(02)00736-9. Bioorg Med Chem Lett. 2002. PMID: 12419375
319 results