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Page 1
Conformationally biased P3 amide replacements of beta-secretase inhibitors.
Stachel SJ, Coburn CA, Steele TG, Crouthamel MC, Pietrak BL, Lai MT, Holloway MK, Munshi SK, Graham SL, Vacca JP. Stachel SJ, et al. Among authors: vacca jp. Bioorg Med Chem Lett. 2006 Feb;16(3):641-4. doi: 10.1016/j.bmcl.2005.10.032. Epub 2005 Nov 2. Bioorg Med Chem Lett. 2006. PMID: 16263281
L-687,908, a potent hydroxyethylene-containing HIV protease inhibitor.
Vacca JP, Guare JP, deSolms SJ, Sanders WM, Giuliani EA, Young SD, Darke PL, Zugay J, Sigal IS, Schleif WA, et al. Vacca JP, et al. J Med Chem. 1991 Mar;34(3):1225-8. doi: 10.1021/jm00107a050. J Med Chem. 1991. PMID: 2002465 No abstract available.
Potent noncovalent thrombin inhibitors that utilize the unique amino acid D-dicyclohexylalanine in the P3 position. Implications on oral bioavailability and antithrombotic efficacy.
Tucker TJ, Lumma WC, Lewis SD, Gardell SJ, Lucas BJ, Baskin EP, Woltmann R, Lynch JJ, Lyle EA, Appleby SD, Chen IW, Dancheck KB, Vacca JP. Tucker TJ, et al. Among authors: vacca jp. J Med Chem. 1997 May 23;40(11):1565-9. doi: 10.1021/jm970140s. J Med Chem. 1997. PMID: 9171866
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. Among authors: vacca jp. J Med Chem. 1997 Oct 24;40(22):3687-93. doi: 10.1021/jm970397q. J Med Chem. 1997. PMID: 9357536
Discovery of a novel, selective, and orally bioavailable class of thrombin inhibitors incorporating aminopyridyl moieties at the P1 position.
Feng DM, Gardell SJ, Lewis SD, Bock MG, Chen Z, Freidinger RM, Naylor-Olsen AM, Ramjit HG, Woltmann R, Baskin EP, Lynch JJ, Lucas R, Shafer JA, Dancheck KB, Chen IW, Mao SS, Krueger JA, Hare TR, Mulichak AM, Vacca JP. Feng DM, et al. Among authors: vacca jp. J Med Chem. 1997 Nov 7;40(23):3726-33. doi: 10.1021/jm970493r. J Med Chem. 1997. PMID: 9371237
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: vacca jp. J Med Chem. 1998 Jan 29;41(3):401-6. doi: 10.1021/jm9705014. J Med Chem. 1998. PMID: 9464370
132 results