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Page 1
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: egbertson ms. 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
Design and synthesis of 8-hydroxy-[1,6]naphthyridines as novel inhibitors of HIV-1 integrase in vitro and in infected cells.
Zhuang L, Wai JS, Embrey MW, Fisher TE, Egbertson MS, Payne LS, Guare JP Jr, Vacca JP, Hazuda DJ, Felock PJ, Wolfe AL, Stillmock KA, Witmer MV, Moyer G, Schleif WA, Gabryelski LJ, Leonard YM, Lynch JJ Jr, Michelson SR, Young SD. Zhuang L, et al. Among authors: egbertson ms. J Med Chem. 2003 Feb 13;46(4):453-6. doi: 10.1021/jm025553u. J Med Chem. 2003. PMID: 12570367
A naphthyridine carboxamide provides evidence for discordant resistance between mechanistically identical inhibitors of HIV-1 integrase.
Hazuda DJ, Anthony NJ, Gomez RP, Jolly SM, Wai JS, Zhuang L, Fisher TE, Embrey M, Guare JP Jr, Egbertson MS, Vacca JP, Huff JR, Felock PJ, Witmer MV, Stillmock KA, Danovich R, Grobler J, Miller MD, Espeseth AS, Jin L, Chen IW, Lin JH, Kassahun K, Ellis JD, Wong BK, Xu W, Pearson PG, Schleif WA, Cortese R, Emini E, Summa V, Holloway MK, Young SD. Hazuda DJ, et al. Among authors: egbertson ms. Proc Natl Acad Sci U S A. 2004 Aug 3;101(31):11233-8. doi: 10.1073/pnas.0402357101. Epub 2004 Jul 26. Proc Natl Acad Sci U S A. 2004. PMID: 15277684 Free PMC article.
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. 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
Diketo acid inhibitor mechanism and HIV-1 integrase: implications for metal binding in the active site of phosphotransferase enzymes.
Grobler JA, Stillmock K, Hu B, Witmer M, Felock P, Espeseth AS, Wolfe A, Egbertson M, Bourgeois M, Melamed J, Wai JS, Young S, Vacca J, Hazuda DJ. Grobler JA, et al. Proc Natl Acad Sci U S A. 2002 May 14;99(10):6661-6. doi: 10.1073/pnas.092056199. Epub 2002 May 7. Proc Natl Acad Sci U S A. 2002. PMID: 11997448 Free PMC article.
4-Aryl-2,4-dioxobutanoic acid inhibitors of HIV-1 integrase and viral replication in cells.
Wai JS, Egbertson MS, Payne LS, Fisher TE, Embrey MW, Tran LO, Melamed JY, Langford HM, Guare JP Jr, Zhuang L, Grey VE, Vacca JP, Holloway MK, Naylor-Olsen AM, Hazuda DJ, Felock PJ, Wolfe AL, Stillmock KA, Schleif WA, Gabryelski LJ, Young SD. Wai JS, et al. Among authors: egbertson ms. J Med Chem. 2000 Dec 28;43(26):4923-6. doi: 10.1021/jm000176b. J Med Chem. 2000. PMID: 11150161 No abstract available.
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
24 results