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28 results

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Page 1
Low molecular weight thrombin inhibitors with excellent potency, metabolic stability, and oral bioavailability.
Morrissette MM, Stauffer KJ, Williams PD, Lyle TA, Vacca JP, Krueger JA, Lewis SD, Lucas BJ, Wong BK, White RB, Miller-Stein C, Lyle EA, Wallace AA, Leonard YM, Welsh DC, Lynch JJ, McMasters DR. Morrissette MM, et al. Among authors: lyle ta, lyle ea. Bioorg Med Chem Lett. 2004 Aug 16;14(16):4161-4. doi: 10.1016/j.bmcl.2004.06.030. Bioorg Med Chem Lett. 2004. PMID: 15261262
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: lyle ta, lyle ea. J Med Chem. 2003 Feb 13;46(4):461-73. doi: 10.1021/jm020311f. J Med Chem. 2003. PMID: 12570369
Pharmacokinetic optimization of 3-amino-6-chloropyrazinone acetamide thrombin inhibitors. Implementation of P3 pyridine N-oxides to deliver an orally bioavailable series containing P1 N-benzylamides.
Burgey CS, Robinson KA, Lyle TA, Nantermet PG, Selnick HG, Isaacs RC, Lewis SD, Lucas BJ, Krueger JA, Singh R, Miller-Stein C, White RB, Wong B, Lyle EA, Stranieri MT, Cook JJ, McMasters DR, Pellicore JM, Pal S, Wallace AA, Clayton FC, Bohn D, Welsh DC, Lynch JJ Jr, Yan Y, Chen Z, Kuo L, Gardell SJ, Shafer JA, Vacca JP. Burgey CS, et al. Among authors: lyle ta, lyle ea. Bioorg Med Chem Lett. 2003 Apr 7;13(7):1353-7. doi: 10.1016/s0960-894x(03)00099-4. Bioorg Med Chem Lett. 2003. PMID: 12657281
P2 pyridine N-oxide thrombin inhibitors: a novel peptidomimetic scaffold.
Nantermet PG, Burgey CS, Robinson KA, Pellicore JM, Newton CL, Deng JZ, Selnick HG, Lewis SD, Lucas BJ, Krueger JA, Miller-Stein C, White RB, Wong B, McMasters DR, Wallace AA, Lynch JJ Jr, Yan Y, Chen Z, Kuo L, Gardell SJ, Shafer JA, Vacca JP, Lyle TA. Nantermet PG, et al. Among authors: lyle ta. Bioorg Med Chem Lett. 2005 Jun 2;15(11):2771-5. doi: 10.1016/j.bmcl.2005.03.110. Bioorg Med Chem Lett. 2005. PMID: 15911253
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: lyle ta. 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
10-Hydroxy-7,8-dihydropyrazino[1',2':1,5]pyrrolo[2,3-d]pyridazine-1,9(2H,6H)-diones: potent, orally bioavailable HIV-1 integrase strand-transfer inhibitors with activity against integrase mutants.
Wiscount CM, Williams PD, Tran LO, Embrey MW, Fisher TE, Sherman V, Homnick CF, Donnette Staas D, Lyle TA, Wai JS, Vacca JP, Wang Z, Felock PJ, Stillmock KA, Witmer MV, Miller MD, Hazuda DJ, Day AM, Gabryelski LJ, Ecto LT, Schleif WA, DiStefano DJ, Kochansky CJ, Anari MR. Wiscount CM, et al. Among authors: lyle ta. Bioorg Med Chem Lett. 2008 Aug 15;18(16):4581-3. doi: 10.1016/j.bmcl.2008.07.037. Epub 2008 Jul 15. Bioorg Med Chem Lett. 2008. PMID: 18657970
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: lyle ta, lyle ea. J Med Chem. 1998 Nov 5;41(23):4466-74. doi: 10.1021/jm980368v. J Med Chem. 1998. PMID: 9804686
Dihydroxypyridopyrazine-1,6-dione HIV-1 integrase inhibitors.
Wai JS, Kim B, Fisher TE, Zhuang L, Embrey MW, Williams PD, Staas DD, Culberson C, Lyle TA, Vacca JP, Hazuda DJ, Felock PJ, Schleif WA, Gabryelski LJ, Jin L, Chen IW, Ellis JD, Mallai R, Young SD. Wai JS, et al. Among authors: lyle ta. Bioorg Med Chem Lett. 2007 Oct 15;17(20):5595-9. doi: 10.1016/j.bmcl.2007.07.092. Epub 2007 Aug 22. Bioorg Med Chem Lett. 2007. PMID: 17822898
28 results