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Synthesis of a series of potent and orally bioavailable thrombin inhibitors that utilize 3,3-disubstituted propionic acid derivatives in the P3 position.
Tucker TJ, Lumma WC, Lewis SD, Gardell SJ, Lucas BJ, Sisko JT, Lynch JJ, Lyle EA, Baskin EP, Woltmann RF, Appleby SD, Chen IW, Dancheck KB, Naylor-Olsen AM, Krueger JA, Cooper CM, Vacca JP. Tucker TJ, et al. J Med Chem. 1997 Oct 24;40(22):3687-93. doi: 10.1021/jm970397q. J Med Chem. 1997. PMID: 9357536
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. J Med Chem. 1998 Aug 13;41(17):3210-9. doi: 10.1021/jm9801713. J Med Chem. 1998. PMID: 9703466
Identification and SAR for a selective, nonpeptidyl thrombin inhibitor.
Naylor-Olsen AM, Ponticello GS, Lewis SD, Mulichak AM, Chen Z, Habecker CN, Phillips BT, Sanders WM, Tucker TJ, Shafer JA, Vacca JP. Naylor-Olsen AM, et al. Among authors: tucker tj. Bioorg Med Chem Lett. 1998 Jul 7;8(13):1697-702. doi: 10.1016/s0960-894x(98)00296-0. Bioorg Med Chem Lett. 1998. PMID: 9873418
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
Tucker TJ, Sisko JT, Tynebor RM, Williams TM, Felock PJ, Flynn JA, Lai MT, Liang Y, McGaughey G, Liu M, Miller M, Moyer G, Munshi V, Perlow-Poehnelt R, Prasad S, Reid JC, Sanchez R, Torrent M, Vacca JP, Wan BL, Yan Y. Tucker TJ, et al. J Med Chem. 2008 Oct 23;51(20):6503-11. doi: 10.1021/jm800856c. Epub 2008 Oct 1. J Med Chem. 2008. PMID: 18826204
62 results