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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: kim jy. J Med Chem. 2007 Nov 29;50(24):5886-9. doi: 10.1021/jm070708p. Epub 2007 Nov 8. J Med Chem. 2007. PMID: 17988109
Synthesis and SAR of novel conformationally-restricted oxazolidinones possessing gram-positive and fastidious gram-negative antibacterial activity. Part 1: Substituted pyrazoles.
Boyer FE, Vara Prasad JV, Choy AL, Chupak L, Dermyer MR, Ding Q, Huband MD, Jiao W, Kaneko T, Khlebnikov V, Kim JY, Lall MS, Maiti SN, Romero K, Wu X. Boyer FE, et al. Among authors: kim jy. Bioorg Med Chem Lett. 2007 Aug 15;17(16):4694-8. doi: 10.1016/j.bmcl.2007.05.056. Epub 2007 May 24. Bioorg Med Chem Lett. 2007. PMID: 17590334
PF-04859989 as a template for structure-based drug design: identification of new pyrazole series of irreversible KAT II inhibitors with improved lipophilic efficiency.
Dounay AB, Anderson M, Bechle BM, Evrard E, Gan X, Kim JY, McAllister LA, Pandit J, Rong S, Salafia MA, Tuttle JB, Zawadzke LE, Verhoest PR. Dounay AB, et al. Among authors: kim jy. Bioorg Med Chem Lett. 2013 Apr 1;23(7):1961-6. doi: 10.1016/j.bmcl.2013.02.039. Epub 2013 Feb 15. Bioorg Med Chem Lett. 2013. PMID: 23466229
Discovery of Brain-Penetrant, Irreversible Kynurenine Aminotransferase II Inhibitors for Schizophrenia.
Dounay AB, Anderson M, Bechle BM, Campbell BM, Claffey MM, Evdokimov A, Evrard E, Fonseca KR, Gan X, Ghosh S, Hayward MM, Horner W, Kim JY, McAllister LA, Pandit J, Paradis V, Parikh VD, Reese MR, Rong S, Salafia MA, Schuyten K, Strick CA, Tuttle JB, Valentine J, Wang H, Zawadzke LE, Verhoest PR. Dounay AB, et al. Among authors: kim jy. ACS Med Chem Lett. 2012 Jan 25;3(3):187-92. doi: 10.1021/ml200204m. eCollection 2012 Mar 8. ACS Med Chem Lett. 2012. PMID: 24900455 Free PMC article.
Structure-Based Design of Irreversible Human KAT II Inhibitors: Discovery of New Potency-Enhancing Interactions.
Tuttle JB, Anderson M, Bechle BM, Campbell BM, Chang C, Dounay AB, Evrard E, Fonseca KR, Gan X, Ghosh S, Horner W, James LC, Kim JY, McAllister LA, Pandit J, Parikh VD, Rago BJ, Salafia MA, Strick CA, Zawadzke LE, Verhoest PR. Tuttle JB, et al. Among authors: kim jy. ACS Med Chem Lett. 2012 Oct 24;4(1):37-40. doi: 10.1021/ml300237v. eCollection 2013 Jan 10. ACS Med Chem Lett. 2012. PMID: 24900560 Free PMC article.
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