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Items: 19


Monoacylglycerol Lipase Inhibition in Human and Rodent Systems Supports Clinical Evaluation of Endocannabinoid Modulators.

Clapper JR, Henry CL, Niphakis MJ, Knize AM, Coppola AR, Simon GM, Ngo N, Herbst RA, Herbst DM, Reed AW, Cisar JS, Weber OD, Viader A, Alexander JP, Cunningham ML, Jones TK, Fraser IP, Grice CA, Ezekowitz RAB, O'Neill GP, Blankman JL.

J Pharmacol Exp Ther. 2018 Oct 10. pii: jpet.118.252296. doi: 10.1124/jpet.118.252296. [Epub ahead of print]


Identification of ABX-1431, a Selective Inhibitor of Monoacylglycerol Lipase and Clinical Candidate for Treatment of Neurological Disorders.

Cisar JS, Weber OD, Clapper JR, Blankman JL, Henry CL, Simon GM, Alexander JP, Jones TK, Ezekowitz RAB, O'Neill GP, Grice CA.

J Med Chem. 2018 Oct 25;61(20):9062-9084. doi: 10.1021/acs.jmedchem.8b00951. Epub 2018 Aug 23.


Pyrazole-based arylalkyne cathepsin S inhibitors. Part III: modification of P4 region.

Wiener JJ, Wickboldt AT, Nguyen S, Sun S, Rynberg R, Rizzolio M, Karlsson L, Edwards JP, Grice CA.

Bioorg Med Chem Lett. 2013 Feb 15;23(4):1070-4. doi: 10.1016/j.bmcl.2012.12.014. Epub 2012 Dec 21.


Identification of benzofuran central cores for the inhibition of leukotriene A(4) hydrolase.

Eccles W, Blevitt JM, Booker JN, Chrovian CC, Crawford S, de Leon AR, Deng X, Fourie AM, Grice CA, Herman K, Karlsson L, Kearney AM, Lee-Dutra A, Liang J, Luna R, Pippel D, Rao N, Riley JP, Santillán A, Savall B, Tanis VM, Xue X, Young AL.

Bioorg Med Chem Lett. 2013 Feb 1;23(3):811-5. doi: 10.1016/j.bmcl.2012.11.074. Epub 2012 Dec 5.


Azabenzthiazole inhibitors of leukotriene A₄ hydrolase.

Tanis VM, Bacani GM, Blevitt JM, Chrovian CC, Crawford S, De Leon A, Fourie AM, Gomez L, Grice CA, Herman K, Kearney AM, Landry-Bayle AM, Lee-Dutra A, Nelson J, Riley JP, Santillán A Jr, Wiener JJ, Xue X, Young AL.

Bioorg Med Chem Lett. 2012 Dec 15;22(24):7504-11. doi: 10.1016/j.bmcl.2012.10.036. Epub 2012 Oct 17.


Discovery of a novel series of selective HCN1 blockers.

McClure KJ, Maher M, Wu N, Chaplan SR, Eckert WA 3rd, Lee DH, Wickenden AD, Hermann M, Allison B, Hawryluk N, Breitenbucher JG, Grice CA.

Bioorg Med Chem Lett. 2011 Sep 15;21(18):5197-201. doi: 10.1016/j.bmcl.2011.07.051. Epub 2011 Jul 23.


Indole- and benzothiophene-based histamine H3 antagonists.

Santillan A Jr, McClure KJ, Allison BD, Lord B, Boggs JD, Morton KL, Everson AM, Nepomuceno D, Letavic MA, Lee-Dutra A, Lovenberg TW, Carruthers NI, Grice CA.

Bioorg Med Chem Lett. 2010 Nov 1;20(21):6226-30. doi: 10.1016/j.bmcl.2010.08.103. Epub 2010 Aug 27.


Thioether acetamides as P3 binding elements for tetrahydropyrido-pyrazole cathepsin S inhibitors.

Wiener DK, Lee-Dutra A, Bembenek S, Nguyen S, Thurmond RL, Sun S, Karlsson L, Grice CA, Jones TK, Edwards JP.

Bioorg Med Chem Lett. 2010 Apr 1;20(7):2379-82. doi: 10.1016/j.bmcl.2010.01.103. Epub 2010 Feb 8.


Discovery and SAR of novel pyrazole-based thioethers as cathepsin S inhibitors. Part 2: Modification of P3, P4, and P5 regions.

Wiener JJ, Wickboldt AT Jr, Wiener DK, Lee-Dutra A, Edwards JP, Karlsson L, Nguyen S, Sun S, Jones TK, Grice CA.

Bioorg Med Chem Lett. 2010 Apr 1;20(7):2375-8. doi: 10.1016/j.bmcl.2010.01.104. Epub 2010 Feb 1.


Discovery and SAR of novel pyrazole-based thioethers as cathepsin S inhibitors: part 1.

Lee-Dutra A, Wiener DK, Arienti KL, Liu J, Mani N, Ameriks MK, Axe FU, Gebauer D, Desai PJ, Nguyen S, Randal M, Thurmond RL, Sun S, Karlsson L, Edwards JP, Jones TK, Grice CA.

Bioorg Med Chem Lett. 2010 Apr 1;20(7):2370-4. doi: 10.1016/j.bmcl.2010.01.108. Epub 2010 Jan 28.


Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity.

Grice CA, Tays KL, Savall BM, Wei J, Butler CR, Axe FU, Bembenek SD, Fourie AM, Dunford PJ, Lundeen K, Coles F, Xue X, Riley JP, Williams KN, Karlsson L, Edwards JP.

J Med Chem. 2008 Jul 24;51(14):4150-69. doi: 10.1021/jm701575k. Epub 2008 Jun 28.


Tetrahydroindazole inhibitors of bacterial type II topoisomerases. Part 2: SAR development and potency against multidrug-resistant strains.

Wiener JJ, Gomez L, Venkatesan H, Santillán A Jr, Allison BD, Schwarz KL, Shinde S, Tang L, Hack MD, Morrow BJ, Motley ST, Goldschmidt RM, Shaw KJ, Jones TK, Grice CA.

Bioorg Med Chem Lett. 2007 May 15;17(10):2718-22. Epub 2007 Mar 6.


Anti-inflammatory activity of a potent, selective leukotriene A4 hydrolase inhibitor in comparison with the 5-lipoxygenase inhibitor zileuton.

Rao NL, Dunford PJ, Xue X, Jiang X, Lundeen KA, Coles F, Riley JP, Williams KN, Grice CA, Edwards JP, Karlsson L, Fourie AM.

J Pharmacol Exp Ther. 2007 Jun;321(3):1154-60. Epub 2007 Mar 19.


Novel pyrazole derivatives as potent inhibitors of type II topoisomerases. Part 1: synthesis and preliminary SAR analysis.

Gomez L, Hack MD, Wu J, Wiener JJ, Venkatesan H, Santillán A Jr, Pippel DJ, Mani N, Morrow BJ, Motley ST, Shaw KJ, Wolin R, Grice CA, Jones TK.

Bioorg Med Chem Lett. 2007 May 15;17(10):2723-7. Epub 2007 Mar 6.


The SAR of 4-substituted (6,6-bicyclic) piperidine cathepsin S inhibitors.

Grice CA, Tays K, Khatuya H, Gustin DJ, Butler CR, Wei J, Sehon CA, Sun S, Gu Y, Jiang W, Thurmond RL, Karlsson L, Edwards JP.

Bioorg Med Chem Lett. 2006 Apr 15;16(8):2209-12. Epub 2006 Feb 3.


Preparation and biological evaluation of indole, benzimidazole, and thienopyrrole piperazine carboxamides: potent human histamine h(4) antagonists.

Venable JD, Cai H, Chai W, Dvorak CA, Grice CA, Jablonowski JA, Shah CR, Kwok AK, Ly KS, Pio B, Wei J, Desai PJ, Jiang W, Nguyen S, Ling P, Wilson SJ, Dunford PJ, Thurmond RL, Lovenberg TW, Karlsson L, Carruthers NI, Edwards JP.

J Med Chem. 2005 Dec 29;48(26):8289-98.


The first potent and selective non-imidazole human histamine H4 receptor antagonists.

Jablonowski JA, Grice CA, Chai W, Dvorak CA, Venable JD, Kwok AK, Ly KS, Wei J, Baker SM, Desai PJ, Jiang W, Wilson SJ, Thurmond RL, Karlsson L, Edwards JP, Lovenberg TW, Carruthers NI.

J Med Chem. 2003 Sep 11;46(19):3957-60.


Preparation of oxime dual NK(1)/NK(2) antagonists with reduced NK(3) affinity.

Reichard GA, Grice CA, Shih NY, Spitler J, Majmundar S, Wang SD, Paliwal S, Anthes JC, Piwinski JJ.

Bioorg Med Chem Lett. 2002 Sep 2;12(17):2355-8.


Synthesis and structure-activity relationships of oxime neurokinin antagonists: discovery of potent arylamides.

Shih NY, Albanese M, Anthes JC, Carruthers NI, Grice CA, Lin L, Mangiaracina P, Reichard GA, Schwerdt J, Seidl V, Wong SC, Piwinski JJ.

Bioorg Med Chem Lett. 2002 Jan 21;12(2):141-5.


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