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Page 1
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: stranieri mt. 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
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: stranieri mt. 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: stranieri mt. 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
Discovery and development of the novel potent orally active thrombin inhibitor N-(9-hydroxy-9-fluorenecarboxy)prolyl trans-4-aminocyclohexylmethyl amide (L-372,460): coapplication of structure-based design and rapid multiple analogue synthesis on solid support.
Brady SF, Stauffer KJ, Lumma WC, Smith GM, Ramjit HG, Lewis SD, Lucas BJ, Gardell SJ, Lyle EA, Appleby SD, Cook JJ, Holahan MA, Stranieri MT, Lynch JJ Jr, Lin JH, Chen IW, Vastag K, Naylor-Olsen AM, Vacca JP. Brady SF, et al. Among authors: stranieri mt. J Med Chem. 1998 Jan 29;41(3):401-6. doi: 10.1021/jm9705014. J Med Chem. 1998. PMID: 9464370
Design and synthesis of a series of potent and orally bioavailable noncovalent thrombin inhibitors that utilize nonbasic groups in the P1 position.
Tucker TJ, Brady SF, Lumma WC, Lewis SD, Gardell SJ, Naylor-Olsen AM, Yan Y, Sisko JT, Stauffer KJ, Lucas BJ, Lynch JJ, Cook JJ, Stranieri MT, Holahan MA, Lyle EA, Baskin EP, Chen IW, Dancheck KB, Krueger JA, Cooper CM, Vacca JP. Tucker TJ, et al. Among authors: stranieri mt. J Med Chem. 1998 Aug 13;41(17):3210-9. doi: 10.1021/jm9801713. J Med Chem. 1998. PMID: 9703466
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: stranieri mt. J Med Chem. 1998 Nov 5;41(23):4466-74. doi: 10.1021/jm980368v. J Med Chem. 1998. PMID: 9804686
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: stranieri mt. 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
Non-peptide glycoprotein IIb/IIIa inhibitors. 17. Design and synthesis of orally active, long-acting non-peptide fibrinogen receptor antagonists.
Askew BC, Bednar RA, Bednar B, Claremon DA, Cook JJ, McIntyre CJ, Hunt CA, Gould RJ, Lynch RJ, Lynch JJ Jr, Gaul SL, Stranieri MT, Sitko GR, Holahan MA, Glass JD, Hamill T, Gorham LM, Prueksaritanont T, Baldwin JJ, Hartman GD. Askew BC, et al. Among authors: stranieri mt. J Med Chem. 1997 Jun 6;40(12):1779-88. doi: 10.1021/jm9608117. J Med Chem. 1997. PMID: 9191954
Non-peptide GPIIb/IIIa inhibitors. 20. Centrally constrained thienothiophene alpha-sulfonamides are potent, long acting in vivo inhibitors of platelet aggregation.
Egbertson MS, Cook JJ, Bednar B, Prugh JD, Bednar RA, Gaul SL, Gould RJ, Hartman GD, Homnick CF, Holahan MA, Libby LA, Lynch JJ Jr, Lynch RJ, Sitko GR, Stranieri MT, Vassallo LM. Egbertson MS, et al. Among authors: stranieri mt. J Med Chem. 1999 Jul 1;42(13):2409-21. doi: 10.1021/jm980722p. J Med Chem. 1999. PMID: 10395482
25 results