Zobrazeno 1 - 10
of 14
pro vyhledávání: '"Alan G. Benson"'
Autor:
Alan G Benson
Publikováno v:
London Review of Education (2019)
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0301840ac5a59907e2d4dca46be72d6f
https://www.scienceopen.com/document?vid=43c74723-9be8-4cd5-88d1-481ba27f8242
https://www.scienceopen.com/document?vid=43c74723-9be8-4cd5-88d1-481ba27f8242
Autor:
Dean Messing, Brian S. Hickory, Alan G. Benson, Matthew J. Saabye, Jeff Hitchcock, Heather M. Madsen, Devadas Balekudru, Shaun R. Selness, Richard C. Durley, Laura D. Marrufo, Gary D. Anderson, Li Xing, Kevin D. Jerome, Michael Hepperle, Christie Lance Christopher, Rajesh V. Devraj, Elizabeth G. Webb, Thomas Owen, Ravi G. Kurumbail, Edgardo Alvira, Jeffrey L. Hirsch, Joseph B. Monahan, Paul V. Rucker, Boehm Terri L, Blevis-Bal Radhika M, Huey S. Shieh, John K. Walker, John F. Schindler, Michele A. Promo, Win Naing, Sheri L. Bonar
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:4059-4065
A series of N-aryl pyridinone inhibitors of p38 mitogen activated protein (MAP) kinase were designed and prepared based on the screening hit SC-25028 (1) and structural comparisons to VX-745 (5). The focus of the investigation targeted the dependence
Autor:
Dean Messing, Win Naing, Joseph P. Portanova, Tina Kim, Alan G. Benson, Shaun R. Selness, Daniel L. Flynn, Joseph B. Monahan, Richard Lindmark, Huey S. Shieh, John K. Walker, Syaulan Yang, Ravi Kurambail, Rajesh V. Devraj, Michael Hepperle, Dice Tom
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:2634-2638
Starting from an initial HTS screening lead, a novel series of C(5)-substituted diaryl pyrazoles were developed that showed potent inhibition of p38alpha kinase. Key to this outcome was the switch from a pyridyl to pyrimidine at the C(4)-position lea
Autor:
Sandra W. Curtiss, D. Joseph Rogier, Alan MacInnes, Brown David L, Mike B. Tollefson, Brian R. Bond, Yvette M. Fobian, Maddux Todd Michael, Dafydd R. Owen, Jeanne M. Rumsey, Brent V. Mischke, Jerry W. Cubbage, Alan G. Benson, Robert Hughes, Lena L Zhang, E. Jon Jacobsen, Steven E. Heasley, Joseph B. Moon, Ying Yu, John M. Molyneaux, Yi Zheng, Brad A. Acker, Blevis-Bal Radhika M, John N. Freskos, John K. Walker, Jennie L. Walgren
Publikováno v:
Journal of Medicinal Chemistry. 53:2656-2660
We recently described a novel series of aminopyridopyrazinones as PDE5 inhibitors. Efforts toward optimization of this series culminated in the identification of 3-[4-(2-hydroxyethyl)piperazin-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[
Autor:
Maddux Todd Michael, Yvette M. Fobian, Alan G. Benson, Dafydd R. Owen, Brian R. Bond, Christopher Phillips, Brad A. Acker, E. Jon Jacobsen, Michael John Palmer, D. Joseph Rogier, John M. Molyneaux, Brent V. Mischke, John N. Freskos, Tracy J. Ringer, Andrew Simon Bell, Blevis-Bal Radhika M, Robert Hughes, David G. Brown, Steve E. Heasley, Joseph B. Moon, John K. Walker, Brown David L, William C. Stallings, Michael B. Tollefson, Alan MacInnes, Jerry W. Cubbage, Yung Yu, Margarita Rodriquez-Lens, Fox David Nathan Abraham
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:4088-4091
A new class of potent and selective PDE5 inhibitors is disclosed. Guided by X-ray crystallographic data, optimization of an HTS lead led to the discovery of a series of 2-aryl, (N8)-alkyl substituted-6-aminosubstituted pyrido[3,2b]pyrazinones which s
Autor:
Robert O, Hughes, D Joseph, Rogier, E Jon, Jacobsen, John K, Walker, Alan, Macinnes, Brian R, Bond, Lena L, Zhang, Ying, Yu, Yi, Zheng, Jeanne M, Rumsey, Jennie L, Walgren, Sandra W, Curtiss, Yvette M, Fobian, Steven E, Heasley, Jerry W, Cubbage, Joseph B, Moon, David L, Brown, Brad A, Acker, Todd M, Maddux, Mike B, Tollefson, Brent V, Mischke, Dafydd R, Owen, John N, Freskos, John M, Molyneaux, Alan G, Benson, Rhadika M, Blevis-Bal
Publikováno v:
Journal of medicinal chemistry. 53(6)
We recently described a novel series of aminopyridopyrazinones as PDE5 inhibitors. Efforts toward optimization of this series culminated in the identification of 3-[4-(2-hydroxyethyl)piperazin-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[
Autor:
Alan G. Benson, John E. Baldus, Michael Hepperle, Li Xing, Kevin D. Jerome, Shaun R. Selness, John K. Walker, Rajesh V. Devraj
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(10)
The synthesis, structure–activity relationship and modeling of a series of 5-substituted-N-aryl pyridazinone based p38α inhibitors are described. In comparing the series to the similar N-aryl pyridinone series, it was found that the pyridazinones
Autor:
Mike B. Tollefson, Joseph B. Moon, Brent V. Mischke, E. Jon Jacobsen, D. Joseph Rogier, Alan G. Benson, Maddux Todd Michael, Brad A. Acker, Jeanne M. Rumsey, John N. Freskos, Blevis-Bal Radhika M, Alan MacInnes, Yi Zheng, Steve E. Heasley, Brown David L, John K. Walker, Yvette M. Fobian, Dafydd R. Owen, Jerry W. Cubbage, Robert Hughes, Ying Yu, John M. Molyneaux, Brian R. Bond
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(17)
We describe efforts to improve the pharmacokinetic profile of the aminopyridopyrazinone class of PDE5 inhibitors. These efforts led to the discovery of 3-[(trans-4-hydroxycyclohexyl)amino]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyra
Autor:
Jennifer M. Williams, Li Xing, Ravi G. Kurumbail, Devadas Balekudru, Jeffrey L. Hirsch, Alan G. Benson, Heidi R. Hope, Roderick A. Stegeman, Zara Walden, Joseph B. Monahan, Shaun R. Selness, Rajesh V. Devraj, Richard M. Broadus, Huey S. Shieh, John K. Walker, Robert P. Compton, John F. Schindler
Publikováno v:
Biochemistry. 48(27)
PH-797804 is a diarylpyridinone inhibitor of p38alpha mitogen-activated protein (MAP) kinase derived from a racemic mixture as the more potent atropisomer (aS), first proposed by molecular modeling and subsequently confirmed by experiments. On the ba
Autor:
Alan MacInnes, E. Jon Jacobsen, Robert Hughes, Blevis-Bal Radhika M, Jennifer M. Williams, John K. Walker, Joseph B. Moon, Jeanne M. Rumsey, Brad A. Acker, Steve E. Heasley, Maddux Todd Michael, Dafydd R. Owen, Ying Yu, John M. Molyneaux, Jerry W. Cubbage, Brian R. Bond, Brown David L, Alan G. Benson, John N. Freskos, William C. Stallings, Brent V. Mischke, Yvette M. Fobian, D. Joseph Rogier, Yi Zheng, Mike B. Tollefson
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(15)
Efforts to improve the potency and physical properties of the aminopyridiopyrazinone class of PDE5 inhibitors through modification of the core ring system are described. Five new ring systems are evaluated and features that impart improved potency an