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Synthesis of 5-(1-H or 1-alkyl-5-oxopyrrolidin-3-yl)-8-hydroxy-[1,6]-naphthyridine-7-carboxamide inhibitors of HIV-1 integrase.
Melamed JY, Egbertson MS, Varga S, Vacca JP, Moyer G, Gabryelski L, Felock PJ, Stillmock KA, Witmer MV, Schleif W, Hazuda DJ, Leonard Y, Jin L, Ellis JD, Young SD. Melamed JY, et al. Among authors: vacca jp. Bioorg Med Chem Lett. 2008 Oct 1;18(19):5307-10. doi: 10.1016/j.bmcl.2008.08.038. Epub 2008 Aug 14. Bioorg Med Chem Lett. 2008. PMID: 18774711
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.
Metabolism of synthetic inositol trisphosphate analogs.
Polokoff MA, Bencen GH, Vacca JP, deSolms SJ, Young SD, Huff JR. Polokoff MA, et al. Among authors: vacca jp. J Biol Chem. 1988 Aug 25;263(24):11922-7. J Biol Chem. 1988. PMID: 2841338 Free article.
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
132 results