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Page 1
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: hartman gd. ChemMedChem. 2006 Aug;1(8):807-11. doi: 10.1002/cmdc.200600097. ChemMedChem. 2006. PMID: 16902933 No abstract available.
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: hartman gd. J Med Chem. 2004 Nov 18;47(24):5825-8. doi: 10.1021/jm049400d. J Med Chem. 2004. PMID: 15537338
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: hartman gd. 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: hartman gd. 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: hartman gd. 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
Challenges in the development of mGluR5 positive allosteric modulators: the discovery of CPPHA.
Zhao Z, Wisnoski DD, O'Brien JA, Lemaire W, Williams DL Jr, Jacobson MA, Wittman M, Ha SN, Schaffhauser H, Sur C, Pettibone DJ, Duggan ME, Conn PJ, Hartman GD, Lindsley CW. Zhao Z, et al. Among authors: hartman gd. Bioorg Med Chem Lett. 2007 Mar 1;17(5):1386-91. doi: 10.1016/j.bmcl.2006.11.081. Epub 2006 Dec 3. Bioorg Med Chem Lett. 2007. PMID: 17210250
Discovery of a potent, CNS-penetrant orexin receptor antagonist based on an n,n-disubstituted-1,4-diazepane scaffold that promotes sleep in rats.
Whitman DB, Cox CD, Breslin MJ, Brashear KM, Schreier JD, Bogusky MJ, Bednar RA, Lemaire W, Bruno JG, Hartman GD, Reiss DR, Harrell CM, Kraus RL, Li Y, Garson SL, Doran SM, Prueksaritanont T, Li C, Winrow CJ, Koblan KS, Renger JJ, Coleman PJ. Whitman DB, et al. Among authors: hartman gd. ChemMedChem. 2009 Jul;4(7):1069-74. doi: 10.1002/cmdc.200900069. ChemMedChem. 2009. PMID: 19418500
169 results