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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: sanderson pe. J Med Chem. 2003 Feb 13;46(4):461-73. doi: 10.1021/jm020311f. J Med Chem. 2003. PMID: 12570369
Discovery of potent, selective 4-fluoroproline-based thrombin inhibitors with improved metabolic stability.
Staas DD, Savage KL, Sherman VL, Shimp HL, Lyle TA, Tran LO, Wiscount CM, McMasters DR, Sanderson PE, Williams PD, Lucas BJ Jr, Krueger JA, Lewis SD, White RB, Yu S, Wong BK, Kochansky CJ, Anari MR, Yan Y, Vacca JP. Staas DD, et al. Among authors: sanderson pe. Bioorg Med Chem. 2006 Oct 15;14(20):6900-16. doi: 10.1016/j.bmc.2006.06.040. Epub 2006 Jul 25. Bioorg Med Chem. 2006. PMID: 16870455
Thrombin inhibitor design.
Sanderson PE, Naylor-Olsen AM. Sanderson PE, et al. Curr Med Chem. 1998 Aug;5(4):289-304. Curr Med Chem. 1998. PMID: 9668196 Review.
Efficacious, orally bioavailable thrombin inhibitors based on 3-aminopyridinone or 3-aminopyrazinone acetamide peptidomimetic templates.
Sanderson PE, Lyle TA, Cutrona KJ, Dyer DL, Dorsey BD, McDonough CM, Naylor-Olsen AM, Chen IW, Chen Z, Cook JJ, Cooper CM, Gardell SJ, Hare TR, Krueger JA, Lewis SD, Lin JH, Lucas BJ Jr, Lyle EA, Lynch JJ Jr, Stranieri MT, Vastag K, Yan Y, Shafer JA, Vacca JP. Sanderson PE, et al. J Med Chem. 1998 Nov 5;41(23):4466-74. doi: 10.1021/jm980368v. J Med Chem. 1998. PMID: 9804686
L-374,087, an efficacious, orally bioavailable, pyridinone acetamide thrombin inhibitor.
Sanderson PE, Cutrona KJ, Dorsey BD, Dyer DL, McDonough CM, Naylor-Olsen AM, Chen IW, Chen Z, Cook JJ, Gardell SJ, Krueger JA, Lewis SD, Lin JH, Lucas BJ Jr, Lyle EA, Lynch JJ Jr, Stranieri MT, Vastag K, Shafer JA, Vacca JP. Sanderson PE, et al. Bioorg Med Chem Lett. 1998 Apr 7;8(7):817-22. doi: 10.1016/s0960-894x(98)00117-6. Bioorg Med Chem Lett. 1998. PMID: 9871547
C6 modification of the pyridinone core of thrombin inhibitor L-374,087 as a means of enhancing its oral absorption.
Isaacs RC, Cutrona KJ, Newton CL, Sanderson PE, Solinsky MG, Baskin EP, Chen IW, Cooper CM, Cook JJ, Gardell SJ, Lewis SD, Lucas RJ Jr, Lyle EA, Lynch JJ Jr, Naylor-Olsen AM, Stranieri MT, Vastag K, Vacca JP. Isaacs RC, et al. Among authors: sanderson pe. Bioorg Med Chem Lett. 1998 Jul 7;8(13):1719-24. doi: 10.1016/s0960-894x(98)00297-2. Bioorg Med Chem Lett. 1998. PMID: 9873422
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