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Synthesis and evaluation of 2-pyridinone derivatives as HIV-1 specific reverse transcriptase inhibitors. 1. Phthalimidoalkyl and -alkylamino analogues.
Hoffman JM, Wai JS, Thomas CM, Levin RB, O'Brien JA, Goldman ME. Hoffman JM, et al. J Med Chem. 1992 Oct 16;35(21):3784-91. doi: 10.1021/jm00099a006. J Med Chem. 1992. PMID: 1279172
Pharmacology of L-744,453, a novel nonpeptidyl endothelin antagonist.
Williams DL Jr, Murphy KL, Nolan NA, O'Brien JA, Lis EV Jr, Pettibone DJ, Clineschmidt BV, Krause SM, Veber DF, Naylor EM, Chakravarty PK, Walsh TF, Dhanoa DM, Chen A, Bagley SW, Fitch KJ, Greenlee WJ. Williams DL Jr, et al. Life Sci. 1996;58(14):1149-57. doi: 10.1016/0024-3205(96)00073-2. Life Sci. 1996. PMID: 8614266
Pharmacology of L-754,142, a highly potent, orally active, nonpeptidyl endothelin antagonist.
Williams DL Jr, Murphy KL, Nolan NA, O'Brien JA, Pettibone DJ, Kivlighn SD, Krause SM, Lis EV Jr, Zingaro GJ, Gabel RA, et al. Williams DL Jr, et al. J Pharmacol Exp Ther. 1995 Dec;275(3):1518-26. J Pharmacol Exp Ther. 1995. PMID: 8531124
Biotransformation of 5-chloro-3-phenylthioindole-2-carboxamide (L-734,005) in rhesus monkeys and rat liver microsomes to a potent HIV-1 reverse transcriptase inhibitor.
Balani SK, Goldman ME, Kauffman LR, Varga SL, O'Brien JA, Smith SJ, Olah TV, Ramjit HG, Schorn TW, Pitzenberger SM, et al. Balani SK, et al. Drug Metab Dispos. 1993 Jul-Aug;21(4):598-604. Drug Metab Dispos. 1993. PMID: 7690697
A nonnucleoside reverse transcriptase inhibitor active on human immunodeficiency virus type 1 isolates resistant to related inhibitors.
Goldman ME, O'Brien JA, Ruffing TL, Schleif WA, Sardana VV, Byrnes VW, Condra JH, Hoffman JM, Emini EA. Goldman ME, et al. Antimicrob Agents Chemother. 1993 May;37(5):947-9. doi: 10.1128/aac.37.5.947. Antimicrob Agents Chemother. 1993. PMID: 7685996 Free PMC article.
Synthesis of a series of 4-(arylethynyl)-6-chloro-4-cyclopropyl-3,4-dihydroquinazolin-2(1H)-ones as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.
Tucker TJ, Lyle TA, Wiscount CM, Britcher SF, Young SD, Sanders WM, Lumma WC, Goldman ME, O'Brien JA, Ball RG, et al. Tucker TJ, et al. J Med Chem. 1994 Jul 22;37(15):2437-44. doi: 10.1021/jm00041a023. J Med Chem. 1994. PMID: 7520079
Metabolism of 3-[2-(benzoxazol-2-yl)ethyl]-5-ethyl-6-methylpyridin-2 (1H)-one (L-696,229), an HIV-1 reverse transcriptase inhibitor, by rat liver slices and in humans.
Balani SK, Kauffman LR, Arison BH, Olah TV, Goldman ME, Varga SL, O'Brien JA, Ramjit HG, Rooney CS, Hoffman JM, et al. Balani SK, et al. Drug Metab Dispos. 1994 Mar-Apr;22(2):200-5. Drug Metab Dispos. 1994. PMID: 7516852
2-Pyridinone derivatives: a new class of nonnucleoside, HIV-1-specific reverse transcriptase inhibitors.
Saari WS, Hoffman JM, Wai JS, Fisher TE, Rooney CS, Smith AM, Thomas CM, Goldman ME, O'Brien JA, Nunberg JH, et al. Saari WS, et al. J Med Chem. 1991 Sep;34(9):2922-5. doi: 10.1021/jm00113a036. J Med Chem. 1991. PMID: 1716683 No abstract available.
Viral resistance to human immunodeficiency virus type 1-specific pyridinone reverse transcriptase inhibitors.
Nunberg JH, Schleif WA, Boots EJ, O'Brien JA, Quintero JC, Hoffman JM, Emini EA, Goldman ME. Nunberg JH, et al. J Virol. 1991 Sep;65(9):4887-92. doi: 10.1128/JVI.65.9.4887-4892.1991. J Virol. 1991. PMID: 1714522 Free PMC article.
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