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3-Benzyl-1,3-oxazolidin-2-ones as mGluR2 positive allosteric modulators: Hit-to lead and lead optimization.
Duplantier AJ, Efremov I, Candler J, Doran AC, Ganong AH, Haas JA, Hanks AN, Kraus KG, Lazzaro JT Jr, Lu J, Maklad N, McCarthy SA, O'Sullivan TJ, Rogers BN, Siuciak JA, Spracklin DK, Zhang L. Duplantier AJ, et al. Among authors: kraus kg. Bioorg Med Chem Lett. 2009 May 1;19(9):2524-9. doi: 10.1016/j.bmcl.2009.03.032. Epub 2009 Mar 14. Bioorg Med Chem Lett. 2009. PMID: 19328692
Optimization of the physicochemical and pharmacokinetic attributes in a 6-azauracil series of P2X7 receptor antagonists leading to the discovery of the clinical candidate CE-224,535.
Duplantier AJ, Dombroski MA, Subramanyam C, Beaulieu AM, Chang SP, Gabel CA, Jordan C, Kalgutkar AS, Kraus KG, Labasi JM, Mussari C, Perregaux DG, Shepard R, Taylor TJ, Trevena KA, Whitney-Pickett C, Yoon K. Duplantier AJ, et al. Among authors: kraus kg. Bioorg Med Chem Lett. 2011 Jun 15;21(12):3708-11. doi: 10.1016/j.bmcl.2011.04.077. Epub 2011 Apr 24. Bioorg Med Chem Lett. 2011. PMID: 21565499
Biarylcarboxylic acids and -amides: inhibition of phosphodiesterase type IV versus [3H]rolipram binding activity and their relationship to emetic behavior in the ferret.
Duplantier AJ, Biggers MS, Chambers RJ, Cheng JB, Cooper K, Damon DB, Eggler JF, Kraus KG, Marfat A, Masamune H, Pillar JS, Shirley JT, Umland JP, Watson JW. Duplantier AJ, et al. Among authors: kraus kg. J Med Chem. 1996 Jan 5;39(1):120-5. doi: 10.1021/jm9505066. J Med Chem. 1996. PMID: 8568798
1-[(1-methyl-1H-imidazol-2-yl)methyl]-4-phenylpiperidines as mGluR2 positive allosteric modulators for the treatment of psychosis.
Zhang L, Brodney MA, Candler J, Doran AC, Duplantier AJ, Efremov IV, Evrard E, Kraus K, Ganong AH, Haas JA, Hanks AN, Jenza K, Lazzaro JT, Maklad N, McCarthy SA, Qian W, Rogers BN, Rottas MD, Schmidt CJ, Siuciak JA, Tingley FD 3rd, Zhang AQ. Zhang L, et al. J Med Chem. 2011 Mar 24;54(6):1724-39. doi: 10.1021/jm101414h. Epub 2011 Mar 2. J Med Chem. 2011. PMID: 21366332