Publications by authors named "Ronald Magolda"

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The synthesis and biological evaluation of quinolyl-piperazinyl piperidines as potent serotonin 5-HT1A antagonists.
Wayne E Childers, Lisa M Havran, Magda Asselin, James J Bicksler, Dan C Chong, Ronald Magolda

J Med Chem· May 2010

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Pyridinyl aminohydantoins as small molecule BACE1 inhibitors.
Ping Zhou, Yanfang Li, Yi Fan, Zheng Wang, Rajiv Chopra, Ronald L Magolda

Bioorg Med Chem Lett· April 2010

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Design and synthesis of 5,5'-disubstituted aminohydantoins as potent and selective human beta-secretase (BACE1) inhibitors.
Michael S Malamas, Jim Erdei, Iwan Gunawan, Jim Turner, Yun Hu, Ronald L Magolda

J Med Chem· February 2010

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Modulation of Wnt signaling through inhibition of secreted frizzled-related protein I (sFRP-1) with N-substituted piperidinyl diphenylsulfonyl sulfonamides: part II.
William J Moore, Jeffrey C Kern, Ramesh Bhat, Peter V N Bodine, Shoichi Fukyama, Ronald L Magolda

Bioorg Med Chem· January 2010

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Begacestat (GSI-953): a novel, selective thiophene sulfonamide inhibitor of amyloid precursor protein gamma-secretase for the treatment of Alzheimer's disease.
Robert L Martone, Hua Zhou, Kevin Atchison, Thomas Comery, Jane Z Xu, Ronald Magolda

J Pharmacol Exp Ther· November 2009

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(1-(4-(Naphthalen-2-yl)pyrimidin-2-yl)piperidin-4-yl)methanamine: a wingless beta-catenin agonist that increases bone formation rate.
Jeffrey C Pelletier, Joseph T Lundquist, Adam M Gilbert, Nipa Alon, Frederick J Bex, Ronald L Magolda

J Med Chem· November 2009

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Selective Kv1.5 blockers: development of (R)-1-(methylsulfonylamino)-3-[2-(4-methoxyphenyl)ethyl]-4-(4-methoxyphenyl)-2-imidazolidinone (KVI-020/WYE-160020) as a potential treatment for atrial arrhythmia.
Benjamin E Blass, Andrew Fensome, Eugene Trybulski, Ronald Magolda, Stephen J Gardell

J Med Chem· November 2009

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Discovery of 6-({4-[2-(4-tert-butylphenyl)-1H-benzimidazol-4-yl]piperazin-1-yl}methyl)quinoxaline (WAY-207024): an orally active antagonist of the gonadotropin releasing hormone receptor (GnRH-R).
Jeffrey C Pelletier, Murty V Chengalvala, Joshua E Cottom, Irene B Feingold, Daniel M Green, Ronald L Magolda

J Med Chem· April 2009

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Prodrugs of perzinfotel with improved oral bioavailability.
Reinhardt B Baudy, John A Butera, Magid A Abou-Gharbia, Hong Chen, Boyd Harrison, Ronald Magolda

J Med Chem· February 2009

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Modulation of Wnt signaling through inhibition of secreted frizzled-related protein I (sFRP-1) with N-substituted piperidinyl diphenylsulfonyl sulfonamides.
William J Moore, Jeffrey C Kern, Ramesh Bhat, Thomas J Commons, Shoichi Fukayama, Ronald L Magolda

J Med Chem· January 2009

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Indazole-based liver X receptor (LXR) modulators with maintained atherosclerotic lesion reduction activity but diminished stimulation of hepatic triglyceride synthesis.
Jay Wrobel, Robert Steffan, S Marc Bowen, Ronald Magolda, Edward Matelan

J Med Chem· November 2008

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Itk kinase inhibitors: initial efforts to improve the metabolical stability and the cell activity of the benzimidazole lead.
Kevin J Moriarty, Michael Winters, Lei Qiao, Declan Ryan, Renee DesJarlis, Ronald Magolda

Bioorg Med Chem Lett· October 2008

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Discovery, SAR and X-ray structure of 1H-benzimidazole-5-carboxylic acid cyclohexyl-methyl-amides as inhibitors of inducible T-cell kinase (Itk).
Kevin J Moriarty, Hidenori Takahashi, Steven S Pullen, Hnin Hnin Khine, Rosemarie H Sallati, Ronald L Magolda

Bioorg Med Chem Lett· October 2008

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Enhanced clearance of Abeta in brain by sustaining the plasmin proteolysis cascade.
J Steven Jacobsen, Thomas A Comery, Robert L Martone, Hassan Elokdah, David L Crandall, Ronald Magolda

Proc Natl Acad Sci U S A· June 2008

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Binding of rapamycin analogs to calcium channels and FKBP52 contributes to their neuroprotective activities.
Benfang Ruan, Kevin Pong, Flora Jow, Mark Bowlby, Robert A Crozier, Ronald L Magolda

Proc Natl Acad Sci U S A· January 2008

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Novel 1-(azacyclyl)-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines as 5-HT6 agonists and antagonists.
Hassan Elokdah, David Li, Geraldine McFarlane, Ronald C Bernotas, Albert J Robichaud, Ronald L Magolda

Bioorg Med Chem· September 2007

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Discovery and optimization of p38 inhibitors via computer-assisted drug design.
Daniel R Goldberg, Ming-Hong Hao, Kevin C Qian, Alan D Swinamer, Donghong A Gao, Ronald L Magolda

J Med Chem· August 2007

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Discovery of potent and selective PKC-theta inhibitors.
Charles L Cywin, Georg Dahmann, Anthony S Prokopowicz, Erick R R Young, Ronald L Magolda

Bioorg Med Chem Lett· January 2007

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Evolution of the thienopyridine class of inhibitors of IkappaB kinase-beta: part I: hit-to-lead strategies.
Tina Morwick, Angela Berry, Janice Brickwood, Mario Cardozo, Katrina Catron, Ronald Magolda

J Med Chem· May 2006

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Beyond U0126. Dianion chemistry leading to the rapid synthesis of a series of potent MEK inhibitors.
John Wityak, Frank W Hobbs, Daniel S Gardner, Joseph B Santella, Joseph J Petraitis, Ronald L Magolda

Bioorg Med Chem Lett· March 2004

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Rational design, synthesis and structure-activity relationships of a cyclic succinate series of TNF-alpha converting enzyme inhibitors. Part 2: lead optimization.
Chu-Biao Xue, Xiaohua He, John Roderick, Ronald L Corbett, James J-W Duan, Ronald L Magolda

Bioorg Med Chem Lett· December 2003

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Rational design, synthesis and structure-activity relationships of a cyclic succinate series of TNF-alpha converting enzyme inhibitors. Part 1: lead identification.
Chu-Biao Xue, Xiaohua He, John Roderick, Ronald L Corbett, James J-W Duan, Ronald L Magolda

Bioorg Med Chem Lett· December 2003

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Aggrecan protects cartilage collagen from proteolytic cleavage.
Michael A Pratta, Wenqing Yao, Carl Decicco, Micky D Tortorella, Riu-Qin Liu, Ronald Magolda

J Biol Chem· November 2003

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Discovery of N-hydroxy-2-(2-oxo-3-pyrrolidinyl)acetamides as potent and selective inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).
James J-W Duan, Zhonghui Lu, Chu-Biao Xue, Xiaohua He, Jennifer L Seng, Ronald L Magolda

Bioorg Med Chem Lett· June 2003

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Design, synthesis, and evaluation of benzothiadiazepine hydroxamates as selective tumor necrosis factor-alpha converting enzyme inhibitors.
Robert J Cherney, James J-W Duan, Matthew E Voss, Lihua Chen, Li Wang, Ronald L Magolda

J Med Chem· May 2003

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