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Items: 1 to 20 of 109

1.

Design, synthesis, and SAR of N-((1-(4-(propylsulfonyl)piperazin-1-yl)cycloalkyl)methyl)benzamide inhibitors of glycine transporter-1.

Cioffi CL, Wolf MA, Guzzo PR, Sadalapure K, Parthasarathy V, Dethe D, Maeng JH, Carulli E, Loong DT, Fang X, Hu M, Gupta P, Chung M, Bai M, Moore N, Luche M, Khmelnitsky Y, Love PL, Watson MA, Mhyre AJ, Liu S.

Bioorg Med Chem Lett. 2013 Mar 1;23(5):1257-61. doi: 10.1016/j.bmcl.2013.01.006. Epub 2013 Jan 11.

PMID:
23380375
2.

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.

Bioorg Med Chem Lett. 2006 Dec 1;16(23):5968-72. Epub 2006 Sep 20.

PMID:
16987662
3.

Synthesis and Biological Evaluation of N-((1-(4-(Sulfonyl)piperazin-1-yl)cycloalkyl)methyl)benzamide Inhibitors of Glycine Transporter-1.

Cioffi CL, Liu S, Wolf MA, Guzzo PR, Sadalapure K, Parthasarathy V, Loong DT, Maeng JH, Carulli E, Fang X, Kalesh KA, Matta L, Choo SH, Panduga S, Buckle RN, Davis RN, Sakwa SA, Gupta P, Sargent BJ, Moore NA, Luche MM, Carr GJ, Khmelnitsky YL, Ismail J, Chung M, Bai M, Leong WY, Sachdev N, Swaminathan S, Mhyre AJ.

J Med Chem. 2016 Aug 25. [Epub ahead of print]

PMID:
27559615
4.

The discovery of potent glycine transporter type-2 inhibitors: design and synthesis of phenoxymethylbenzamide derivatives.

Takahashi E, Arai T, Akahira M, Nakajima M, Nishimura K, Omori Y, Kumagai H, Suzuki T, Hayashi R.

Bioorg Med Chem Lett. 2014 Sep 15;24(18):4603-6. doi: 10.1016/j.bmcl.2014.06.059. Epub 2014 Jun 27.

PMID:
25176190
5.

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.

ChemMedChem. 2006 Aug;1(8):807-11. No abstract available.

PMID:
16902933
6.

The synthesis and SAR of 2-arylsulfanyl-phenyl piperazinyl acetic acids as glyT-1 inhibitors.

Smith G, Ruhland T, Mikkelsen G, Andersen K, Christoffersen CT, Alifrangis LH, Mørk A, Wren SP, Harris N, Wyman BM, Brandt G.

Bioorg Med Chem Lett. 2004 Aug 2;14(15):4027-30.

PMID:
15225720
7.

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.

Bioorg Med Chem Lett. 2009 Mar 1;19(5):1488-91. doi: 10.1016/j.bmcl.2008.12.115. Epub 2009 Jan 9.

PMID:
19179073
8.

A novel radioligand for glycine transporter 1: characterization and use in autoradiographic and in vivo brain occupancy studies.

Zeng Z, O'Brien JA, Lemaire W, O'Malley SS, Miller PJ, Zhao Z, Wallace MA, Raab C, Lindsley CW, Sur C, Williams DL Jr.

Nucl Med Biol. 2008 Apr;35(3):315-25. doi: 10.1016/j.nucmedbio.2007.12.002.

PMID:
18355687
9.

Inhibitors of GlyT1 affect glycine transport via discrete binding sites.

Mezler M, Hornberger W, Mueller R, Schmidt M, Amberg W, Braje W, Ochse M, Schoemaker H, Behl B.

Mol Pharmacol. 2008 Dec;74(6):1705-15. doi: 10.1124/mol.108.049312. Epub 2008 Sep 24. Erratum in: Mol Pharmacol. 2009 Jan;75(1):258.. Amberg, Martin Schmidt Willi [corrected to Schmidt, Martin]; Amberg, Martin Schmidt Willi [corrected to Amberg, Willi].

10.

The first potent and selective inhibitors of the glycine transporter type 2.

Caulfield WL, Collie IT, Dickins RS, Epemolu O, McGuire R, Hill DR, McVey G, Morphy JR, Rankovic Z, Sundaram H.

J Med Chem. 2001 Aug 16;44(17):2679-82. No abstract available.

PMID:
11495577
12.

Acylglycinamides as inhibitors of glycine transporter type 1.

Blunt R, Porter R, Johns A, Nash D, Puckey G, Wyman P, Herdon H, Teague S, Hadden V, Fontana S, Gordon L.

Bioorg Med Chem Lett. 2011 Oct 15;21(20):6176-9. doi: 10.1016/j.bmcl.2011.07.096. Epub 2011 Aug 6.

PMID:
21889344
13.

Structure-affinity relationship study on N-[4-(4-arylpiperazin-1-yl)butyl]arylcarboxamides as potent and selective dopamine D(3) receptor ligands.

Leopoldo M, Berardi F, Colabufo NA, De Giorgio P, Lacivita E, Perrone R, Tortorella V.

J Med Chem. 2002 Dec 19;45(26):5727-35.

PMID:
12477356
14.

2-(Aminomethyl)-benzamide-based glycine transporter type-2 inhibitors.

Ho KK, Appell KC, Baldwin JJ, Bohnstedt AC, Dong G, Guo T, Horlick R, Islam KR, Kultgen SG, Masterson CM, McDonald E, McMillan K, Morphy JR, Rankovic Z, Sundaram H, Webb M.

Bioorg Med Chem Lett. 2004 Jan 19;14(2):545-8.

PMID:
14698200
15.

Discovery and SAR studies of novel GlyT1 inhibitors.

Walter MW, Hoffman BJ, Gordon K, Johnson K, Love P, Jones M, Man T, Phebus L, Reel JK, Rudyk HC, Shannon H, Svensson K, Yu H, Valli MJ, Porter WJ.

Bioorg Med Chem Lett. 2007 Sep 15;17(18):5233-8. Epub 2007 Jun 30.

PMID:
17629697
16.

Spinal antiallodynia action of glycine transporter inhibitors in neuropathic pain models in mice.

Morita K, Motoyama N, Kitayama T, Morioka N, Kifune K, Dohi T.

J Pharmacol Exp Ther. 2008 Aug;326(2):633-45. doi: 10.1124/jpet.108.136267. Epub 2008 Apr 30.

17.

The discovery of a structurally novel class of inhibitors of the type 1 glycine transporter.

Lowe JA 3rd, Hou X, Schmidt C, David Tingley F 3rd, McHardy S, Kalman M, Deninno S, Sanner M, Ward K, Lebel L, Tunucci D, Valentine J, Bronk BS, Schaeffer E.

Bioorg Med Chem Lett. 2009 Jun 1;19(11):2974-6. doi: 10.1016/j.bmcl.2009.04.035. Epub 2009 Apr 18. Erratum in: Bioorg Med Chem Lett. 2009 Aug 15;19(16):4885. Bronk, Brian S [added]; Schaeffer, Eric [added].

PMID:
19410451
18.

Synthesis and characterization of [¹²⁵I]2-iodo N-[(S)-{(S)-1-methylpiperidin-2-yl}(phenyl)methyl]3-trifluoromethyl-benzamide as novel imaging probe for glycine transporter 1.

Fuchigami T, Haratake M, Magata Y, Haradahira T, Nakayama M.

Bioorg Med Chem. 2011 Nov 1;19(21):6245-53. doi: 10.1016/j.bmc.2011.09.010. Epub 2011 Sep 10.

PMID:
21975065
19.

The synthesis and SAR of 2-arylsulfanylphenyl-1-oxyalkylamino acids as GlyT-1 inhibitors.

Smith G, Mikkelsen G, Eskildsen J, Bundgaard C.

Bioorg Med Chem Lett. 2006 Aug 1;16(15):3981-4. Epub 2006 May 24.

PMID:
16725323
20.

N-[2-[4-(4-Chlorophenyl)piperazin-1-yl]ethyl]-3-methoxybenzamide: a potent and selective dopamine D4 ligand.

Perrone R, Berardi F, Colabufo NA, Leopoldo M, Tortorella V.

J Med Chem. 1998 Nov 19;41(24):4903-9.

PMID:
9822559
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