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Synthesis and bioactivity of novel bis(heteroaryl)piperazine (BHAP) reverse transcriptase inhibitors: structure-activity relationships and increased metabolic stability of novel substituted pyridine analogs.
Genin MJ, Poel TJ, Yagi Y, Biles C, Althaus I, Keiser BJ, Kopta LA, Friis JM, Reusser F, Adams WJ, Olmsted RA, Voorman RL, Thomas RC, Romero DL. Genin MJ, et al. Among authors: romero dl. J Med Chem. 1996 Dec 20;39(26):5267-75. doi: 10.1021/jm960269m. J Med Chem. 1996. PMID: 8978855
Bis(heteroaryl)piperazine (BHAP) reverse transcriptase inhibitors: structure-activity relationships of novel substituted indole analogues and the identification of 1-[(5-methanesulfonamido-1H-indol-2-yl)-carbonyl]-4-[3- [(1-methylethyl)amino]-pyridinyl]piperazine monomethanesulfonate (U-90152S), a second-generation clinical candidate.
Romero DL, Morge RA, Genin MJ, Biles C, Busso M, Resnick L, Althaus IW, Reusser F, Thomas RC, Tarpley WG. Romero DL, et al. J Med Chem. 1993 May 14;36(10):1505-8. doi: 10.1021/jm00062a027. J Med Chem. 1993. PMID: 7684450 No abstract available.
(Alkylamino) piperidine bis(heteroaryl)piperizine analogs are potent, broad-spectrum nonnucleoside reverse transcriptase inhibitors of drug-resistant isolates of human immunodeficiency virus type 1 (HIV-1) and select for drug-resistant variants of HIV-1IIIB with reduced replication phenotypes.
Olmsted RA, Slade DE, Kopta LA, Poppe SM, Poel TJ, Newport SW, Rank KB, Biles C, Morge RA, Dueweke TJ, Yagi Y, Romero DL, Thomas RC, Sharma SK, Tarpley WG. Olmsted RA, et al. Among authors: romero dl. J Virol. 1996 Jun;70(6):3698-705. doi: 10.1128/JVI.70.6.3698-3705.1996. J Virol. 1996. PMID: 8648704 Free PMC article.
Targeting delavirdine/atevirdine resistant HIV-1: identification of (alkylamino)piperidine-containing bis(heteroaryl)piperazines as broad spectrum HIV-1 reverse transcriptase inhibitors.
Romero DL, Olmsted RA, Poel TJ, Morge RA, Biles C, Keiser BJ, Kopta LA, Friis JM, Hosley JD, Stefanski KJ, Wishka DG, Evans DB, Morris J, Stehle RG, Sharma SK, Yagi Y, Voorman RL, Adams WJ, Tarpley WG, Thomas RC. Romero DL, et al. J Med Chem. 1996 Sep 13;39(19):3769-89. doi: 10.1021/jm960158n. J Med Chem. 1996. PMID: 8809165
44 results