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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: lyle ta. 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
Discovery of potent, selective 4-fluoroproline-based thrombin inhibitors with improved metabolic stability.
Staas DD, Savage KL, Sherman VL, Shimp HL, Lyle TA, Tran LO, Wiscount CM, McMasters DR, Sanderson PE, Williams PD, Lucas BJ Jr, Krueger JA, Lewis SD, White RB, Yu S, Wong BK, Kochansky CJ, Anari MR, Yan Y, Vacca JP. Staas DD, et al. Bioorg Med Chem. 2006 Oct 15;14(20):6900-16. doi: 10.1016/j.bmc.2006.06.040. Epub 2006 Jul 25. Bioorg Med Chem. 2006. PMID: 16870455
Dihydroxypyridopyrazine-1,6-dione HIV-1 integrase inhibitors.
Wai JS, Kim B, Fisher TE, Zhuang L, Embrey MW, Williams PD, Staas DD, Culberson C, Lyle TA, Vacca JP, Hazuda DJ, Felock PJ, Schleif WA, Gabryelski LJ, Jin L, Chen IW, Ellis JD, Mallai R, Young SD. Wai JS, et al. Bioorg Med Chem Lett. 2007 Oct 15;17(20):5595-9. doi: 10.1016/j.bmcl.2007.07.092. Epub 2007 Aug 22. Bioorg Med Chem Lett. 2007. PMID: 17822898
8-Hydroxy-3,4-dihydropyrrolo[1,2-a]pyrazine-1(2H)-one HIV-1 integrase inhibitors.
Fisher TE, Kim B, Staas DD, Lyle TA, Young SD, Vacca JP, Zrada MM, Hazuda DJ, Felock PJ, Schleif WA, Gabryelski LJ, Anari MR, Kochansky CJ, Wai JS. Fisher TE, et al. Bioorg Med Chem Lett. 2007 Dec 1;17(23):6511-5. doi: 10.1016/j.bmcl.2007.09.086. Epub 2007 Sep 29. Bioorg Med Chem Lett. 2007. PMID: 17931865
Potent and selective HIV-1 ribonuclease H inhibitors based on a 1-hydroxy-1,8-naphthyridin-2(1H)-one scaffold.
Williams PD, Staas DD, Venkatraman S, Loughran HM, Ruzek RD, Booth TM, Lyle TA, Wai JS, Vacca JP, Feuston BP, Ecto LT, Flynn JA, DiStefano DJ, Hazuda DJ, Bahnck CM, Himmelberger AL, Dornadula G, Hrin RC, Stillmock KA, Witmer MV, Miller MD, Grobler JA. Williams PD, et al. Among authors: lyle ta. Bioorg Med Chem Lett. 2010 Nov 15;20(22):6754-7. doi: 10.1016/j.bmcl.2010.08.135. Epub 2010 Sep 24. Bioorg Med Chem Lett. 2010. PMID: 20869872
Metabolism-directed optimization of 3-aminopyrazinone acetamide thrombin inhibitors. Development of an orally bioavailable series containing P1 and P3 pyridines.
Burgey CS, Robinson KA, Lyle TA, Sanderson PE, Lewis SD, Lucas BJ, Krueger JA, Singh R, Miller-Stein C, White RB, Wong B, Lyle EA, Williams PD, Coburn CA, Dorsey BD, Barrow JC, Stranieri MT, Holahan MA, Sitko GR, Cook JJ, McMasters DR, McDonough CM, Sanders WM, Wallace AA, Clayton FC, Bohn D, Leonard YM, Detwiler TJ Jr, Lynch JJ Jr, Yan Y, Chen Z, Kuo L, Gardell SJ, Shafer JA, Vacca JP. Burgey CS, et al. Among authors: lyle ta, lyle ea. J Med Chem. 2003 Feb 13;46(4):461-73. doi: 10.1021/jm020311f. J Med Chem. 2003. PMID: 12570369
112 results