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Page 1
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: zavadoski wj. 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 a potent glucagon receptor antagonist with favorable physicochemical and pharmacokinetic properties as a candidate for the treatment of type 2 diabetes mellitus.
Guzman-Perez A, Pfefferkorn JA, Lee EC, Stevens BD, Aspnes GE, Bian J, Didiuk MT, Filipski KJ, Moore D, Perreault C, Sammons MF, Tu M, Brown J, Atkinson K, Litchfield J, Tan B, Samas B, Zavadoski WJ, Salatto CT, Treadway J. Guzman-Perez A, et al. Among authors: zavadoski wj. Bioorg Med Chem Lett. 2013 May 15;23(10):3051-8. doi: 10.1016/j.bmcl.2013.03.014. Epub 2013 Mar 13. Bioorg Med Chem Lett. 2013. PMID: 23562063
Discovery of PF-04620110, a Potent, Selective, and Orally Bioavailable Inhibitor of DGAT-1.
Dow RL, Li JC, Pence MP, Gibbs EM, LaPerle JL, Litchfield J, Piotrowski DW, Munchhof MJ, Manion TB, Zavadoski WJ, Walker GS, McPherson RK, Tapley S, Sugarman E, Guzman-Perez A, DaSilva-Jardine P. Dow RL, et al. Among authors: zavadoski wj. ACS Med Chem Lett. 2011 Mar 18;2(5):407-12. doi: 10.1021/ml200051p. eCollection 2011 May 12. ACS Med Chem Lett. 2011. PMID: 24900321 Free PMC article.
Discovery of spirocyclic proline tryptophan hydroxylase-1 inhibitors.
Goldberg DR, De Lombaert S, Aiello R, Bourassa P, Barucci N, Zhang Q, Paralkar V, Valentine J, Zavadoski W. Goldberg DR, et al. Bioorg Med Chem Lett. 2016 Feb 15;26(4):1124-9. doi: 10.1016/j.bmcl.2016.01.064. Epub 2016 Jan 22. Bioorg Med Chem Lett. 2016. PMID: 26821821
Discovery of acyl guanidine tryptophan hydroxylase-1 inhibitors.
Goldberg DR, De Lombaert S, Aiello R, Bourassa P, Barucci N, Zhang Q, Paralkar V, Stein AJ, Valentine J, Zavadoski W. Goldberg DR, et al. Bioorg Med Chem Lett. 2016 Jun 15;26(12):2855-2860. doi: 10.1016/j.bmcl.2016.04.057. Epub 2016 Apr 21. Bioorg Med Chem Lett. 2016. PMID: 27146606
Optimization of spirocyclic proline tryptophan hydroxylase-1 inhibitors.
Goldberg DR, De Lombaert S, Aiello R, Bourassa P, Barucci N, Zhang Q, Paralkar V, Stein AJ, Holt M, Valentine J, Zavadoski W. Goldberg DR, et al. Bioorg Med Chem Lett. 2017 Feb 1;27(3):413-419. doi: 10.1016/j.bmcl.2016.12.053. Epub 2016 Dec 23. Bioorg Med Chem Lett. 2017. PMID: 28041831
5-Chloroindoloyl glycine amide inhibitors of glycogen phosphorylase: synthesis, in vitro, in vivo, and X-ray crystallographic characterization.
Wright SW, Rath VL, Genereux PE, Hageman DL, Levy CB, McClure LD, McCoid SC, McPherson RK, Schelhorn TM, Wilder DE, Zavadoski WJ, Gibbs EM, Treadway JL. Wright SW, et al. Among authors: zavadoski wj. Bioorg Med Chem Lett. 2005 Jan 17;15(2):459-65. doi: 10.1016/j.bmcl.2004.10.048. Bioorg Med Chem Lett. 2005. PMID: 15603973
18 results