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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: michener mt. 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
Design, synthesis and SAR of a series of 1,3,5-trisubstituted benzenes as thrombin inhibitors.
Isaacs RC, Newton CL, Cutrona KJ, Mercer SP, Payne LS, Stauffer KJ, Williams PD, Cook JJ, Krueger JA, Lewis SD, Lucas BJ, Lyle EA, Lynch JJ, McMasters DR, Naylor-Olsen AM, Michener MT, Wallace AA. Isaacs RC, et al. Among authors: michener mt. Bioorg Med Chem Lett. 2011 Mar 1;21(5):1536-40. doi: 10.1016/j.bmcl.2010.12.105. Epub 2010 Dec 28. Bioorg Med Chem Lett. 2011. PMID: 21295467