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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. Among authors: perlow d. 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
A potent and orally active HIV-1 integrase inhibitor.
Egbertson MS, Moritz HM, Melamed JY, Han W, Perlow DS, Kuo MS, Embrey M, Vacca JP, Zrada MM, Cortes AR, Wallace A, Leonard Y, Hazuda DJ, Miller MD, Felock PJ, Stillmock KA, Witmer MV, Schleif W, Gabryelski LJ, Moyer G, Ellis JD, Jin L, Xu W, Braun MP, Kassahun K, Tsou NN, Young SD. Egbertson MS, et al. Among authors: perlow ds. Bioorg Med Chem Lett. 2007 Mar 1;17(5):1392-8. doi: 10.1016/j.bmcl.2006.11.080. Epub 2006 Dec 3. Bioorg Med Chem Lett. 2007. PMID: 17194584
Nonpeptide oxytocin antagonists: analogs of L-371,257 with improved potency.
Williams PD, Bock MG, Evans BE, Freidinger RM, Gallicchio SN, Guidotti MT, Jacobson MA, Kuo MS, Levy MR, Lis EV, Michelson SR, Pawluczyk JM, Perlow DS, Pettibone DJ, Quigley AG, Reiss DR, Salvatore C, Stauffer KJ, Woyden CJ. Williams PD, et al. Among authors: perlow ds. Bioorg Med Chem Lett. 1999 May 3;9(9):1311-6. doi: 10.1016/s0960-894x(99)00181-x. Bioorg Med Chem Lett. 1999. PMID: 10340620
Conformationally constrained o-tolylpiperazine camphorsulfonamide oxytocin antagonists. Structural modifications that provide high receptor affinity and suggest a bioactive conformation.
Williams PD, Ball RG, Clineschmidt BV, Culberson JC, Erb JM, Freidinger RM, Pawluczyk JM, Perlow DS, Pettibone DJ, Veber DF. Williams PD, et al. Among authors: perlow ds. Bioorg Med Chem. 1994 Sep;2(9):971-85. doi: 10.1016/s0968-0896(00)82046-5. Bioorg Med Chem. 1994. PMID: 7712132
Design and discovery in the development of long-acting renin inhibitors.
Veber DF, Payne LS, Williams PD, Perlow DS, Lundell GF, Gould NP, Siegl PK, Sweet CS, Freidinger RM. Veber DF, et al. Among authors: perlow ds. Biochem Soc Trans. 1990 Dec;18(6):1291-4. doi: 10.1042/bst0181291. Biochem Soc Trans. 1990. PMID: 2088926 No abstract available.
31 results