Search Results - "GRICE, Cheryl A"

Identification of ABX-1431, a Selective Inhibitor of Monoacylglycerol Lipase and Clinical Candidate for Treatment of Neurological Disorders by Cisar, Justin S, Weber, Olivia D, Clapper, Jason R, Blankman, Jacqueline L, Henry, Cassandra L, Simon, Gabriel M, Alexander, Jessica P, Jones, Todd K, Ezekowitz, R. Alan B, O’Neill, Gary P, Grice, Cheryl A

“…The serine hydrolase monoacylglycerol lipase (MGLL) converts the endogenous cannabinoid receptor agonist 2-arachidonoylglycerol (2-AG) and other…”
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Anti-inflammatory activity of a potent, selective leukotriene A4 hydrolase inhibitor in comparison with the 5-lipoxygenase inhibitor zileuton by Rao, Navin L, Dunford, Paul J, Xue, Xiaohua, Jiang, Xiaohui, Lundeen, Katherine A, Coles, Fawn, Riley, Jason P, Williams, Kacy N, Grice, Cheryl A, Edwards, James P, Karlsson, Lars, Fourie, Anne M

“…Leukotriene A(4) hydrolase (LTA(4)H) catalyzes production of the proinflammatory lipid mediator, leukotriene (LT) B(4), which is implicated in a number of…”
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Identification of benzofuran central cores for the inhibition of leukotriene A4 hydrolase by Eccles, Wendy, Blevitt, Jonathan M., Booker, Jamila N., Chrovian, Christa C., Crawford, Shelby, de Leon, Aimee Rose, Deng, Xiaohu, Fourie, Anne M., Grice, Cheryl A., Herman, Krystal, Karlsson, Lars, Kearney, Aaron M., Lee-Dutra, Alice, Liang, Jimmy, Luna, Rosa, Pippel, Dan, Rao, Navin, Riley, Jason P., Santillán, Alejandro, Savall, Brad, Tanis, Virginia M., Xue, Xiaohua, Young, Arlene L.

“…Leukotrienes (LT’s) are known to play a physiological role in inflammatory immune response. Leukotriene A4 hydrolase (LTA4H) is a cystolic enzyme that…”
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Novel pyrazole derivatives as potent inhibitors of type II topoisomerases. Part 1: Synthesis and preliminary SAR analysis by Gomez, Laurent, Hack, Michael D., Wu, Jiejun, Wiener, John J.M., Venkatesan, Hari, Santillán, Alejandro, Pippel, Daniel J., Mani, Neelakandha, Morrow, Brian J., Motley, S. Timothy, Shaw, Karen Joy, Wolin, Ronald, Grice, Cheryl A., Jones, Todd K.

“…In an attempt to search for a new class of antibacterial agents, we have discovered a series of pyrazole analogs that possess good antibacterial activity for…”
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The First Potent and Selective Non-Imidazole Human Histamine H4 Receptor Antagonists by Jablonowski, Jill A, Grice, Cheryl A, Chai, Wenying, Dvorak, Curt A, Venable, Jennifer D, Kwok, Annette K, Ly, Kiev S, Wei, Jianmei, Baker, Sherry M, Desai, Pragnya J, Jiang, Wen, Wilson, Sandy J, Thurmond, Robin L, Karlsson, Lars, Edwards, James P, Lovenberg, Timothy W, Carruthers, Nicholas I

“…Following the discovery of the human histamine H4 receptor, a high throughput screen of our corporate compound collection identified compound 6 as a potential…”
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Preparation and Biological Evaluation of Indole, Benzimidazole, and Thienopyrrole Piperazine Carboxamides:  Potent Human Histamine H4 Antagonists by Venable, Jennifer D, Cai, Hui, Chai, Wenying, Dvorak, Curt A, Grice, Cheryl A, Jablonowski, Jill A, Shah, Chandra R, Kwok, Annette K, Ly, Kiev S, Pio, Barbara, Wei, Jianmei, Desai, Pragnya J, Jiang, Wen, Nguyen, Steven, Ling, Ping, Wilson, Sandy J, Dunford, Paul J, Thurmond, Robin L, Lovenberg, Timothy W, Karlsson, Lars, Carruthers, Nicholas I, Edwards, James P

“…Three series of H4 receptor ligands, derived from indoly-2-yl-(4-methyl-piperazin-1-yl)-methanones, have been synthesized and their structure−activity…”
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Discovery of a novel series of selective HCN1 blockers by McClure, Kelly J., Maher, Michael, Wu, Nancy, Chaplan, Sandra R., Eckert, William A., Lee, Dong H., Wickenden, Alan D., Hermann, Michelle, Allison, Brett, Hawryluk, Natalie, Breitenbucher, J. Guy, Grice, Cheryl A.

“…Identification of some selective and potent HCN1 blockers is described. The discovery of a series of novel, potent, and selective blockers of the cyclic…”
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Tetrahydroindazole inhibitors of bacterial type II topoisomerases. Part 2: SAR development and potency against multidrug-resistant strains by Wiener, John J.M., Gomez, Laurent, Venkatesan, Hariharan, Santillán, Alejandro, Allison, Brett D., Schwarz, Kimberly L., Shinde, Shirin, Tang, Liu, Hack, Michael D., Morrow, Brian J., Motley, S. Timothy, Goldschmidt, Raul M., Shaw, Karen Joy, Jones, Todd K., Grice, Cheryl A.

“…We have previously reported a novel class of tetrahydroindazoles that display potency against a variety of Gram-positive and Gram-negative bacteria,…”
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Pyrazole-based arylalkyne Cathepsin S inhibitors. Part III: Modification of P4 region by Wiener, John J.M., Wickboldt, Alvah Tyson, Nguyen, Steven, Sun, Siquan, Rynberg, Raymond, Rizzolio, Michele, Karlsson, Lars, Edwards, James P., Grice, Cheryl A.

“…Novel classes of tetrahydropyrido-pyrazole thioether amines and arylalkynes that display potency against human Cathepsin S have been previously reported. Here,…”
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Identification of benzofuran central cores for the inhibition of leukotriene A(4) hydrolase by Eccles, Wendy, Blevitt, Jonathan M, Booker, Jamila N, Chrovian, Christa C, Crawford, Shelby, de Leon, Aimee Rose, Deng, Xiaohu, Fourie, Anne M, Grice, Cheryl A, Herman, Krystal, Karlsson, Lars, Kearney, Aaron M, Lee-Dutra, Alice, Liang, Jimmy, Luna, Rosa, Pippel, Dan, Rao, Navin, Riley, Jason P, Santillán, Alejandro, Savall, Brad, Tanis, Virginia M, Xue, Xiaohua, Young, Arlene L

“…Leukotrienes (LT's) are known to play a physiological role in inflammatory immune response. Leukotriene A(4) hydrolase (LTA(4)H) is a cystolic enzyme that…”
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Azabenzthiazole inhibitors of leukotriene A4 hydrolase by Tanis, Virginia M., Bacani, Genesis M., Blevitt, Jonathan M., Chrovian, Christa C., Crawford, Shelby, De Leon, Aimee, Fourie, Anne M., Gomez, Laurent, Grice, Cheryl A., Herman, Krystal, Kearney, Aaron M., Landry-Bayle, Adrienne M., Lee-Dutra, Alice, Nelson, Jay, Riley, Jason P., Santillán, Alejandro, Wiener, John J.M., Xue, Xiaohua, Young, Arlene L.

“…Previously, benzthiazole containing LTA4H inhibitors were discovered that were potent (1–3), but were associated with the potential for a hERG liability…”
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Indole- and benzothiophene-based histamine H3 antagonists by SANTILLAN, Alejandro, MCCLURE, Kelly J, LOVENBERG, Timothy W, CARRUTHERS, Nicholas I, GRICE, Cheryl A, ALLISON, Brett D, LORD, Brian, BOGGS, Jamin D, MORTON, Kirsten L, EVERSON, Anita M, NEPOMUCENO, Diane, LETAVIC, Michael A, LEE-DUTRA, Alice

“…Previous research on histamine H(3) antagonists has led to the development of a pharmacophore model consisting of a central phenyl core flanked by two…”
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Thioether acetamides as P3 binding elements for tetrahydropyrido-pyrazole cathepsin S inhibitors by Wiener, Danielle K., Lee-Dutra, Alice, Bembenek, Scott, Nguyen, Steven, Thurmond, Robin L., Sun, Siquan, Karlsson, Lars, Grice, Cheryl A., Jones, Todd K., Edwards, James P.

“…Pyrazole-based thioether amide inhibitors of cathepsin S: SAR investigations. A series of tetrahydropyrido-pyrazole cathepsin S (CatS) inhibitors with…”
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Discovery and SAR of novel pyrazole-based thioethers as cathepsin S inhibitors. Part 2: Modification of P3, P4, and P5 regions by Wiener, John J.M., Wickboldt, Alvah T., Wiener, Danielle K., Lee-Dutra, Alice, Edwards, James P., Karlsson, Lars, Nguyen, Steven, Sun, Siquan, Jones, Todd K., Grice, Cheryl A.

“…A novel class of tetrahydropyrido-pyrazole thioether amines that display potency against human Cathepsin S have been previously reported. Here, further SAR…”
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Practical Segregation of Incompatible Reagents in the Organic Chemistry Laboratory by Wiener, John J. M, Grice, Cheryl A

“…A new protocol of incompatible chemical reagent segregation has been developed. Serving as a second-level segregation beyond typical first-level separation of…”
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Discovery and SAR of novel pyrazole-based thioethers as cathepsin S inhibitors: Part 1 by Lee-Dutra, Alice, Wiener, Danielle K., Arienti, Kristen L., Liu, Jing, Mani, Neelakandha, Ameriks, Michael K., Axe, Frank U., Gebauer, Damara, Desai, Pragnya J., Nguyen, Steven, Randal, Mike, Thurmond, Robin L., Sun, Siquan, Karlsson, Lars, Edwards, James P., Jones, Todd K., Grice, Cheryl A.

“…A series of pyrazole-based thioethers were prepared and found to be potent cathepsin S inhibitors. A crystal structure of 13 suggests that the thioether moiety…”
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Identification of a Potent, Selective, and Orally Active Leukotriene A4 Hydrolase Inhibitor with Anti-Inflammatory Activity by Grice, Cheryl A, Tays, Kevin L, Savall, Brad M, Wei, Jianmei, Butler, Christopher R, Axe, Frank U, Bembenek, Scott D, Fourie, Anne M, Dunford, Paul J, Lundeen, Katherine, Coles, Fawn, Xue, Xiaohua, Riley, Jason P, Williams, Kacy N, Karlsson, Lars, Edwards, James P

“…LTA4H is a ubiquitously distributed 69 kDa zinc-containing cytosolic enzyme with both hydrolase and aminopeptidase activity. As a hydrolase, LTA4H…”
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The SAR of 4-substituted (6,6-bicyclic) piperidine cathepsin S inhibitors by Grice, Cheryl A., Tays, Kevin, Khatuya, Haripada, Gustin, Darin J., Butler, Christopher R., Wei, Jianmei, Sehon, Clark A., Sun, Siquan, Gu, Yin, Jiang, Wen, Thurmond, Robin L., Karlsson, Lars, Edwards, James P.

“…Noncovalent, potent, and selective inhibitors of the cysteine protease cathepsin S are reported. A series of competitive, reversible cathepsin S (CatS)…”
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Preparation of oxime dual NK1/NK2 antagonists with reduced NK3 affinity by REICHARD, Gregory A, GRICE, Cheryl A, SHIH, Neng-Yang, SPITLER, James, MAJMUNDAR, Sapna, WANG, Steven D, PALIWAL, Sunil, ANTHES, John C, PIWINSKI, John J

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Synthesis and structure–activity relationships of oxime neurokinin antagonists: discovery of potent arylamides by Shih, Neng-Yang, Albanese, Margaret, Anthes, John C, Carruthers, Nicholas I, Grice, Cheryl A, Lin, Ling, Mangiaracina, Pietro, Reichard, Gregory A, Schwerdt, John, Seidl, Vera, Wong, Shing-Chung, Piwinski, John J

“…The structural modification of the benzylic ether region of oxime 1 has resulted in the identification of several novel aryl amides as selective or dual NK…”
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