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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. Among authors: mcdonough cm. J Med Chem. 1998 Nov 5;41(23):4466-74. doi: 10.1021/jm980368v. J Med Chem. 1998. PMID: 9804686
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: mcdonough cm. J Med Chem. 2003 Feb 13;46(4):461-73. doi: 10.1021/jm020311f. J Med Chem. 2003. PMID: 12570369
P3 optimization of functional potency, in vivo efficacy and oral bioavailability in 3-aminopyrazinone thrombin inhibitors bearing non-charged groups at the P1 position.
Isaacs RC, Newton CL, Cutrona KJ, Mercer SP, Dorsey BD, McDonough CM, Cook JJ, Krueger JA, Lewis SD, Lucas BJ, Lyle EA, Lynch JJ, Miller-Stein C, Michener MT, Wallace AA, White RB, Wong BK. Isaacs RC, et al. Among authors: mcdonough cm. Bioorg Med Chem Lett. 2011 Mar 1;21(5):1532-5. doi: 10.1016/j.bmcl.2010.12.108. Epub 2010 Dec 28. Bioorg Med Chem Lett. 2011. PMID: 21295466
Identification of MK-944a: a second clinical candidate from the hydroxylaminepentanamide isostere series of HIV protease inhibitors.
Dorsey BD, McDonough C, McDaniel SL, Levin RB, Newton CL, Hoffman JM, Darke PL, Zugay-Murphy JA, Emini EA, Schleif WA, Olsen DB, Stahlhut MW, Rutkowski CA, Kuo LC, Lin JH, Chen IW, Michelson SR, Holloway MK, Huff JR, Vacca JP. Dorsey BD, et al. J Med Chem. 2000 Sep 7;43(18):3386-99. doi: 10.1021/jm9903848. J Med Chem. 2000. PMID: 10978186
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. Among authors: mcdonough cm. 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
Heel Pain - Plantar Fasciitis: Revision 2023.
Koc TA Jr, Bise CG, Neville C, Carreira D, Martin RL, McDonough CM. Koc TA Jr, et al. Among authors: mcdonough cm. J Orthop Sports Phys Ther. 2023 Dec;53(12):CPG1-CPG39. doi: 10.2519/jospt.2023.0303. J Orthop Sports Phys Ther. 2023. PMID: 38037331 Review.
83 results