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Page 1
9-hydroxyazafluorenes and their use in thrombin inhibitors.
Stauffer KJ, Williams PD, Selnick HG, Nantermet PG, Newton CL, Homnick CF, Zrada MM, Lewis SD, Lucas BJ, Krueger JA, Pietrak BL, Lyle EA, Singh R, Miller-Stein C, White RB, Wong B, Wallace AA, Sitko GR, Cook JJ, Holahan MA, Stranieri-Michener M, Leonard YM, Lynch JJ Jr, McMasters DR, Yan Y. Stauffer KJ, et al. Among authors: holahan ma. J Med Chem. 2005 Apr 7;48(7):2282-93. doi: 10.1021/jm049423s. J Med Chem. 2005. PMID: 15801822
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: holahan ma. J Med Chem. 2003 Feb 13;46(4):461-73. doi: 10.1021/jm020311f. J Med Chem. 2003. PMID: 12570369
Rapid P1 SAR of brain penetrant tertiary carbinamine derived BACE inhibitors.
Zhu H, Young MB, Nantermet PG, Graham SL, Colussi D, Lai MT, Pietrak B, Price EA, Sankaranarayanan S, Shi XP, Tugusheva K, Holahan MA, Michener MS, Cook JJ, Simon A, Hazuda DJ, Vacca JP, Rajapakse HA. Zhu H, et al. Among authors: holahan ma. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1779-82. doi: 10.1016/j.bmcl.2010.01.005. Epub 2010 Jan 11. Bioorg Med Chem Lett. 2010. PMID: 20122828
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: holahan ma. J Med Chem. 1997 Jun 6;40(12):1779-88. doi: 10.1021/jm9608117. J Med Chem. 1997. PMID: 9191954
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: holahan ma. 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: holahan ma. J Med Chem. 1998 Aug 13;41(17):3210-9. doi: 10.1021/jm9801713. J Med Chem. 1998. PMID: 9703466
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: holahan ma. J Med Chem. 1999 Jul 1;42(13):2409-21. doi: 10.1021/jm980722p. J Med Chem. 1999. PMID: 10395482
Methyl-substitution of an iminohydantoin spiropiperidine β-secretase (BACE-1) inhibitor has a profound effect on its potency.
Egbertson M, McGaughey GB, Pitzenberger SM, Stauffer SR, Coburn CA, Stachel SJ, Yang W, Barrow JC, Neilson LA, McWherter M, Perlow D, Fahr B, Munshi S, Allison TJ, Holloway K, Selnick HG, Yang Z, Swestock J, Simon AJ, Sankaranarayanan S, Colussi D, Tugusheva K, Lai MT, Pietrak B, Haugabook S, Jin L, Chen IW, Holahan M, Stranieri-Michener M, Cook JJ, Vacca J, Graham SL. Egbertson M, et al. Bioorg Med Chem Lett. 2015 Nov 1;25(21):4812-4819. doi: 10.1016/j.bmcl.2015.06.082. Epub 2015 Jun 29. Bioorg Med Chem Lett. 2015. PMID: 26195137
Alpha-hydroxy amides as a novel class of bradykinin B1 selective antagonists.
Wood MR, Schirripa KM, Kim JJ, Kuduk SD, Chang RK, Di Marco CN, DiPardo RM, Wan BL, Murphy KL, Ransom RW, Chang RS, Holahan MA, Cook JJ, Lemaire W, Mosser SD, Bednar RA, Tang C, Prueksaritanont T, Wallace AA, Mei Q, Yu J, Bohn DL, Clayton FC, Adarayn ED, Sitko GR, Leonard YM, Freidinger RM, Pettibone DJ, Bock MG. Wood MR, et al. Among authors: holahan ma. Bioorg Med Chem Lett. 2008 Jan 15;18(2):716-20. doi: 10.1016/j.bmcl.2007.11.050. Epub 2007 Nov 19. Bioorg Med Chem Lett. 2008. PMID: 18061443
56 results