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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: lin jh. 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 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: lin jh. 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
Indinavir analogues with blocked metabolism sites as HIV protease inhibitors with improved pharmacological profiles and high potency against PI-resistant viral strains.
Cheng Y, Zhang F, Rano TA, Lu Z, Schleif WA, Gabryelski L, Olsen DB, Stahlhut M, Rutkowski CA, Lin JH, Jin L, Emini EA, Chapman KT, Tata JR. Cheng Y, et al. Among authors: lin jh. Bioorg Med Chem Lett. 2002 Sep 2;12(17):2419-22. doi: 10.1016/s0960-894x(02)00424-9. Bioorg Med Chem Lett. 2002. PMID: 12161147
Orally bioavailable highly potent HIV protease inhibitors against PI-resistant virus.
Lu Z, Bohn J, Rano T, Rutkowski CA, Simcoe AL, Olsen DB, Schleif WA, Carella A, Gabryelski L, Jin L, Lin JH, Emini E, Chapman K, Tata JR. Lu Z, et al. Among authors: lin jh. Bioorg Med Chem Lett. 2005 Dec 1;15(23):5311-4. doi: 10.1016/j.bmcl.2005.08.072. Epub 2005 Oct 3. Bioorg Med Chem Lett. 2005. PMID: 16203148
Identification of MK-944a: a second clinical candidate from the hydroxylaminepentanamide isostere series of HIV protease inhibitors.
Dorsey BD, McDonough C, McDaniel SL, Levin RB, Newton CL, Hoffman JM, Darke PL, Zugay-Murphy JA, Emini EA, Schleif WA, Olsen DB, Stahlhut MW, Rutkowski CA, Kuo LC, Lin JH, Chen IW, Michelson SR, Holloway MK, Huff JR, Vacca JP. Dorsey BD, et al. Among authors: lin jh. J Med Chem. 2000 Sep 7;43(18):3386-99. doi: 10.1021/jm9903848. J Med Chem. 2000. PMID: 10978186
2,007 results