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Page 1
Discovery of positive allosteric modulators for the metabotropic glutamate receptor subtype 5 from a series of N-(1,3-diphenyl-1H- pyrazol-5-yl)benzamides that potentiate receptor function in vivo.
Lindsley CW, Wisnoski DD, Leister WH, O'brien JA, Lemaire W, Williams DL Jr, Burno M, Sur C, Kinney GG, Pettibone DJ, Tiller PR, Smith S, Duggan ME, Hartman GD, Conn PJ, Huff JR. Lindsley CW, et al. Among authors: tiller pr. J Med Chem. 2004 Nov 18;47(24):5825-8. doi: 10.1021/jm049400d. J Med Chem. 2004. PMID: 15537338
A novel selective positive allosteric modulator of metabotropic glutamate receptor subtype 5 has in vivo activity and antipsychotic-like effects in rat behavioral models.
Kinney GG, O'Brien JA, Lemaire W, Burno M, Bickel DJ, Clements MK, Chen TB, Wisnoski DD, Lindsley CW, Tiller PR, Smith S, Jacobson MA, Sur C, Duggan ME, Pettibone DJ, Conn PJ, Williams DL Jr. Kinney GG, et al. Among authors: tiller pr. J Pharmacol Exp Ther. 2005 Apr;313(1):199-206. doi: 10.1124/jpet.104.079244. Epub 2004 Dec 17. J Pharmacol Exp Ther. 2005. PMID: 15608073
Design, synthesis, and in vivo efficacy of glycine transporter-1 (GlyT1) inhibitors derived from a series of [4-phenyl-1-(propylsulfonyl)piperidin-4-yl]methyl benzamides.
Lindsley CW, Zhao Z, Leister WH, O'Brien J, Lemaire W, Williams DL Jr, Chen TB, Chang RS, Burno M, Jacobson MA, Sur C, Kinney GG, Pettibone DJ, Tiller PR, Smith S, Tsou NN, Duggan ME, Conn PJ, Hartman GD. Lindsley CW, et al. Among authors: tiller pr. ChemMedChem. 2006 Aug;1(8):807-11. doi: 10.1002/cmdc.200600097. ChemMedChem. 2006. PMID: 16902933 No abstract available.
Synthesis and SAR of GlyT1 inhibitors derived from a series of N-((4-(morpholine-4-carbonyl)-1-(propylsulfonyl)piperidin-4-yl)methyl)benzamides.
Zhao Z, O'Brien JA, Lemaire W, Williams DL Jr, Jacobson MA, Sur C, Pettibone DJ, Tiller PR, Smith S, Hartman GD, Wolkenberg SE, Lindsley CW. Zhao Z, et al. Among authors: tiller pr. Bioorg Med Chem Lett. 2006 Dec 1;16(23):5968-72. doi: 10.1016/j.bmcl.2006.08.131. Epub 2006 Sep 20. Bioorg Med Chem Lett. 2006. PMID: 16987662
Discovery of N-{[1-(propylsulfonyl)-4-pyridin-2-ylpiperidin-4-yl]methyl}benzamides as novel, selective and potent GlyT1 inhibitors.
Zhao Z, Leister WH, O'Brien JA, Lemaire W, Williams DL Jr, Jacobson MA, Sur C, Kinney GG, Pettibone DJ, Tiller PR, Smith S, Hartman GD, Lindsley CW, Wolkenberg SE. Zhao Z, et al. Among authors: tiller pr. Bioorg Med Chem Lett. 2009 Mar 1;19(5):1488-91. doi: 10.1016/j.bmcl.2008.12.115. Epub 2009 Jan 9. Bioorg Med Chem Lett. 2009. PMID: 19179073
Discovery of GlyT1 inhibitors with improved pharmacokinetic properties.
Wolkenberg SE, Zhao Z, Wisnoski DD, Leister WH, O'Brien J, Lemaire W, Williams DL Jr, Jacobson MA, Sur C, Kinney GG, Pettibone DJ, Tiller PR, Smith S, Gibson C, Ma BK, Polsky-Fisher SL, Lindsley CW, Hartman GD. Wolkenberg SE, et al. Among authors: tiller pr. Bioorg Med Chem Lett. 2009 Mar 1;19(5):1492-5. doi: 10.1016/j.bmcl.2009.01.015. Epub 2009 Jan 10. Bioorg Med Chem Lett. 2009. PMID: 19181525
Synthesis and evaluation of imidazole acetic acid inhibitors of activated thrombin-activatable fibrinolysis inhibitor as novel antithrombotics.
Barrow JC, Nantermet PG, Stauffer SR, Ngo PL, Steinbeiser MA, Mao SS, Carroll SS, Bailey C, Colussi D, Bosserman M, Burlein C, Cook JJ, Sitko G, Tiller PR, Miller-Stein CM, Rose M, McMasters DR, Vacca JP, Selnick HG. Barrow JC, et al. Among authors: tiller pr. J Med Chem. 2003 Dec 4;46(25):5294-7. doi: 10.1021/jm034141y. J Med Chem. 2003. PMID: 14640538
Fast LC/MS in the analysis of small molecules.
Tiller PR, Romanyshyn LA, Neue UD. Tiller PR, et al. Anal Bioanal Chem. 2003 Nov;377(5):788-802. doi: 10.1007/s00216-003-2146-0. Epub 2003 Aug 6. Anal Bioanal Chem. 2003. PMID: 12904948 Review.
36 results