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Antibacterial oxazolidinones possessing a novel C-5 side chain. (5R)-trans-3-[3-Fluoro-4- (1-oxotetrahydrothiopyran-4-yl)phenyl]-2- oxooxazolidine-5-carboxylic acid amide (PF-00422602), a new lead compound.
Poel TJ, Thomas RC, Adams WJ, Aristoff PA, Barbachyn MR, Boyer FE, Brieland J, Brideau R, Brodfuehrer J, Brown AP, Choy AL, Dermyer M, Dority M, Ford CW, Gadwood RC, Hanna D, Hongliang C, Huband MD, Huber C, Kelly R, Kim JY, Martin JP Jr, Pagano PJ, Ross D, Skerlos L, Sulavik MC, Zhu T, Zurenko GE, Prasad JV. Poel TJ, et al. Among authors: thomas rc. J Med Chem. 2007 Nov 29;50(24):5886-9. doi: 10.1021/jm070708p. Epub 2007 Nov 8. J Med Chem. 2007. PMID: 17988109
Identification of phenylisoxazolines as novel and viable antibacterial agents active against Gram-positive pathogens.
Barbachyn MR, Cleek GJ, Dolak LA, Garmon SA, Morris J, Seest EP, Thomas RC, Toops DS, Watt W, Wishka DG, Ford CW, Zurenko GE, Hamel JC, Schaadt RD, Stapert D, Yagi BH, Adams WJ, Friis JM, Slatter JG, Sams JP, Oien NL, Zaya MJ, Wienkers LC, Wynalda MA. Barbachyn MR, et al. Among authors: thomas rc. J Med Chem. 2003 Jan 16;46(2):284-302. doi: 10.1021/jm020248u. J Med Chem. 2003. PMID: 12519066
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. Among authors: thomas rc. J Med Chem. 1996 Sep 13;39(19):3769-89. doi: 10.1021/jm960158n. J Med Chem. 1996. PMID: 8809165
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: thomas rc. J Med Chem. 1996 Dec 20;39(26):5267-75. doi: 10.1021/jm960269m. J Med Chem. 1996. PMID: 8978855
(-)-6-Chloro-2-[(1-furo[2, 3-c]pyridin-5-ylethyl)thio]-4-pyrimidinamine, PNU-142721, a new broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitor.
Wishka DG, Graber DR, Kopta LA, Olmsted RA, Friis JM, Hosley JD, Adams WJ, Seest EP, Castle TM, Dolak LA, Keiser BJ, Yagi Y, Jeganathan A, Schlachter ST, Murphy MJ, Cleek GJ, Nugent RA, Poppe SM, Swaney SM, Han F, Watt W, White WL, Poel TJ, Thomas RC, Morris J, et al. Wishka DG, et al. Among authors: thomas rc. J Med Chem. 1998 Apr 23;41(9):1357-60. doi: 10.1021/jm9801049. J Med Chem. 1998. PMID: 9554867 No abstract available.
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. Among authors: thomas rc. J Med Chem. 1993 May 14;36(10):1505-8. doi: 10.1021/jm00062a027. J Med Chem. 1993. PMID: 7684450 No abstract available.
The benzylthio-pyrimidine U-31,355, a potent inhibitor of HIV-1 reverse transcriptase.
Althaus IW, Chou KC, Lemay RJ, Franks KM, Deibel MR, Kezdy FJ, Resnick L, Busso ME, So AG, Downey KM, Romero DL, Thomas RC, Aristoff PA, Tarpley WG, Reusser F. Althaus IW, et al. Among authors: thomas rc. Biochem Pharmacol. 1996 Mar 22;51(6):743-50. doi: 10.1016/0006-2952(95)02390-9. Biochem Pharmacol. 1996. PMID: 8602869 Free article.
241 results