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Page 1
Discovery and synthesis of HIV integrase inhibitors: development of potent and orally bioavailable N-methyl pyrimidones.
Gardelli C, Nizi E, Muraglia E, Crescenzi B, Ferrara M, Orvieto F, Pace P, Pescatore G, Poma M, Ferreira Mdel R, Scarpelli R, Homnick CF, Ikemoto N, Alfieri A, Verdirame M, Bonelli F, Paz OG, Taliani M, Monteagudo E, Pesci S, Laufer R, Felock P, Stillmock KA, Hazuda D, Rowley M, Summa V. Gardelli C, et al. Among authors: felock p. J Med Chem. 2007 Oct 4;50(20):4953-75. doi: 10.1021/jm0704705. Epub 2007 Sep 8. J Med Chem. 2007. PMID: 17824681
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: felock pj. J Med Chem. 2003 Feb 13;46(4):453-6. doi: 10.1021/jm025553u. J Med Chem. 2003. PMID: 12570367
A series of 5-(5,6)-dihydrouracil substituted 8-hydroxy-[1,6]naphthyridine-7-carboxylic acid 4-fluorobenzylamide inhibitors of HIV-1 integrase and viral replication in cells.
Embrey MW, Wai JS, Funk TW, Homnick CF, Perlow DS, Young SD, Vacca JP, Hazuda DJ, Felock PJ, Stillmock KA, Witmer MV, Moyer G, Schleif WA, Gabryelski LJ, Jin L, Chen IW, Ellis JD, Wong BK, Lin JH, Leonard YM, Tsou NN, Zhuang L. Embrey MW, et al. Among authors: felock pj. Bioorg Med Chem Lett. 2005 Oct 15;15(20):4550-4. doi: 10.1016/j.bmcl.2005.06.105. Bioorg Med Chem Lett. 2005. PMID: 16102965
A series of 5-aminosubstituted 4-fluorobenzyl-8-hydroxy-[1,6]naphthyridine-7-carboxamide HIV-1 integrase inhibitors.
Guare JP, Wai JS, Gomez RP, Anthony NJ, Jolly SM, Cortes AR, Vacca JP, Felock PJ, Stillmock KA, Schleif WA, Moyer G, Gabryelski LJ, Jin L, Chen IW, Hazuda DJ, Young SD. Guare JP, et al. Among authors: felock pj. Bioorg Med Chem Lett. 2006 Jun 1;16(11):2900-4. doi: 10.1016/j.bmcl.2006.03.003. Epub 2006 Mar 22. Bioorg Med Chem Lett. 2006. PMID: 16554152
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: felock pj. 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
10-Hydroxy-7,8-dihydropyrazino[1',2':1,5]pyrrolo[2,3-d]pyridazine-1,9(2H,6H)-diones: potent, orally bioavailable HIV-1 integrase strand-transfer inhibitors with activity against integrase mutants.
Wiscount CM, Williams PD, Tran LO, Embrey MW, Fisher TE, Sherman V, Homnick CF, Donnette Staas D, Lyle TA, Wai JS, Vacca JP, Wang Z, Felock PJ, Stillmock KA, Witmer MV, Miller MD, Hazuda DJ, Day AM, Gabryelski LJ, Ecto LT, Schleif WA, DiStefano DJ, Kochansky CJ, Anari MR. Wiscount CM, et al. Among authors: felock pj. Bioorg Med Chem Lett. 2008 Aug 15;18(16):4581-3. doi: 10.1016/j.bmcl.2008.07.037. Epub 2008 Jul 15. Bioorg Med Chem Lett. 2008. PMID: 18657970
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: felock pj. 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
53 results