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Metabolism-directed optimization of 3-aminopyrazinone acetamide thrombin inhibitors. Development of an orally bioavailable series containing P1 and P3 pyridines.
Burgey CS, Robinson KA, Lyle TA, Sanderson PE, Lewis SD, Lucas BJ, Krueger JA, Singh R, Miller-Stein C, White RB, Wong B, Lyle EA, Williams PD, Coburn CA, Dorsey BD, Barrow JC, Stranieri MT, Holahan MA, Sitko GR, Cook JJ, McMasters DR, McDonough CM, Sanders WM, Wallace AA, Clayton FC, Bohn D, Leonard YM, Detwiler TJ Jr, Lynch JJ Jr, Yan Y, Chen Z, Kuo L, Gardell SJ, Shafer JA, Vacca JP. Burgey CS, et al. Among authors: sanders wm. J Med Chem. 2003 Feb 13;46(4):461-73. doi: 10.1021/jm020311f. J Med Chem. 2003. PMID: 12570369
Identification and SAR for a selective, nonpeptidyl thrombin inhibitor.
Naylor-Olsen AM, Ponticello GS, Lewis SD, Mulichak AM, Chen Z, Habecker CN, Phillips BT, Sanders WM, Tucker TJ, Shafer JA, Vacca JP. Naylor-Olsen AM, et al. Among authors: sanders wm. Bioorg Med Chem Lett. 1998 Jul 7;8(13):1697-702. doi: 10.1016/s0960-894x(98)00296-0. Bioorg Med Chem Lett. 1998. PMID: 9873418
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