Zobrazeno 1 - 8
of 8
pro vyhledávání: '"Kenneth C. Rupert"'
Autor:
Brian C. Shook, Kenneth C. Rupert, Stefanie Rassnick, Hall Daniel A, Scott Davis, Sandra Damon, Reyes Mayra B, Lori Westover, Melville C. Osborne, Scott Youells, Yuting Tang, Ronald K. Russell, Keith T. Demarest, Xun Li, Paul F. Jackson, Shawn Branum, Devraj Chakravarty, Derek A. Beauchamp, Kristin Hansen, Kenneth J. Rhodes, David C. Palmer, James L. Bullington, Geoffrey R. Heintzelman, Kenneth M. Wells, Jamie Boulet
Publikováno v:
Journal of Medicinal Chemistry. 53:8104-8115
The in vivo characterization of a dual adenosine A(2A)/A(1) receptor antagonist in several animal models of Parkinson's disease is described. Discovery and scale-up syntheses of compound 1 are described in detail, highlighting optimization steps that
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f4a3abc6b1bb2388ce859a84328d2aeb
https://doi.org/10.1021/jm100971t
https://doi.org/10.1021/jm100971t
Autor:
Sandra Damon, Lori Westover, Kenneth C. Rupert, Ronald K. Russell, Xun Li, Devraj Chakravarty, Paul F. Jackson, Brian Magliaro, Yuting Tang, Geoffrey R. Heintzelman, Kenneth M. Wells, Stefanie Rassnick, Shawn Branum, Mel Osbourne, Karen Carroll, Kenneth J. Rhodes, James L. Bullington, Robert H. Scannevin, Keith T. Demarest, Lisa Lampron, Brian C. Shook, Scott Youells, Kristen Hansen, Hall Daniel A
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:2864-2867
A novel series of arylindenopyrimidines were identified as A(2A) and A(1) receptor antagonists. The series was optimized for in vitro activity by substituting the 8- and 9-positions with methylene amine substituents. The compounds show excellent acti
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f81d5b2a5b35b6c6aec43edf95869ec0
https://doi.org/10.1016/j.bmcl.2010.03.042
https://doi.org/10.1016/j.bmcl.2010.03.042
Autor:
Scott Youells, Robert H. Scannevin, Mark T. Powell, Sandra Damon, Ronald K. Russell, Paul F. Jackson, Lori Westover, Lisa Lampron, Jeffrey Crooke, Karen Carroll, Kristen Hansen, Geoffrey R. Heintzelman, Kenneth M. Wells, Kenneth J. Rhodes, J. Kent Barbay, N. H. Wallace, Devraj Chakravarty, Stefanie Rassnick, Brian C. Shook, Aihua Wang, Hall Daniel A, Kenneth C. Rupert, Xun Li, Vernon C. Alford, Derek A. Beauchamp, Shawn Branum, Kristi A. Leonard, Mark Ault, James L. Bullington
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:2868-2871
Two reactive metabolites were identified in vivo for the dual A2A/A1 receptor antagonist 1. Two strategies were implemented to successfully mitigate the metabolic liabilities associated with 1. Optimization of the arylindenopyrimidines led to a numbe
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::353b6f972a700b3aa70793fd134b85a1
https://doi.org/10.1016/j.bmcl.2010.03.024
https://doi.org/10.1016/j.bmcl.2010.03.024
Publikováno v:
Organometallics. 21:144-149
A new class of chiral indenes (verbenindenes), in which a verbenone moiety is annulated to an indene core, is prepared by a sequence of Shapiro lithiation and Nazarov cyclization reactions. Since the initial indenes are resistant to deprotonation, th
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::c0079dc5e4860d571184c49f9a176f2f
https://doi.org/10.1021/om010731n
https://doi.org/10.1021/om010731n
Autor:
Henry James Robert, Druie Cavender, Peter H. Schafer, John H. Dodd, Ignatius J. Turchi, Scott A. Wadsworth, John Siekierka, Kenneth C. Rupert
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 8:3335-3340
The MAP kinase p38 plays a key role in the biosynthesis of the inflammatory cytokines TNF-alpha and IL-1. We have developed a novel series of potent p38 inhibitors that could lead to new methods of treatment for inflammatory diseases such as rheumato
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e0c7690305f8385de3871c7647fad8c1
https://doi.org/10.1016/s0960-894x(98)00589-7
https://doi.org/10.1016/s0960-894x(98)00589-7
Autor:
Peter H. Schafer, Kenneth C. Rupert, Scott A. Wadsworth, John Siekierka, Ignatius J. Turchi, John H. Dodd, Druie Cavender, Henry James Robert
Publikováno v:
ChemInform. 30
The MAP kinase p38 plays a key role in the biosynthesis of the inflammatory cytokines TNF-α and IL-1. We have developed a novel series of potent p38 inhibitors that could lead to new methods of treatment for inflammatory diseases such as rheumatoid
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::e00bdf559f283966740b486a1f8ffc0b
https://doi.org/10.1002/chin.199911166
https://doi.org/10.1002/chin.199911166
Autor:
Xun Li, Bangping Xiang, Kristin M. Averill, Wai Ping Leung, Bohumila Fahmy, Paul F. Jackson, Dennis C. Argentieri, Hall Daniel A, John Siekierka, Xiaodong Fan, Thomas Razler, James L. Bullington, Gilbert C. Olini, Michael Reuman, Ping Ling, Demetrius Carter, Russell Wolff, Geoffrey R. Heintzelman, Druie Cavender, Scott A. Wadsworth, Kenneth C. Rupert, Ronald K. Russell, Yue Mei Zhang
Publikováno v:
Bioorganicmedicinal chemistry letters. 16(23)
Inhibition of the p38 map kinase pathway has been shown to be beneficial in the treatment of inflammatory diseases. The first class of potent p38 kinase inhibitors was the pyridinylimidazole compounds from SKB. Since then several pyridinylimidazole-b
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2d98c9f8328eb28109b2118bac61f3c5
https://pubmed.ncbi.nlm.nih.gov/16971122
https://pubmed.ncbi.nlm.nih.gov/16971122
Autor:
Gilbert C. Olini, Bohumila Fahmy, Henry James Robert, John Siekierka, Druie Cavender, John H. Dodd, Kenneth C. Rupert, Scott A. Wadsworth
Publikováno v:
ChemInform. 34
The MAP kinase p38 is implicated in the release of the pro-inflammatory cytokines TNF-alpha and IL-1 beta. Inhibition of cytokine release may be a useful treatment for inflammatory conditions such as rheumatoid arthritis and Crohn's disease. A novel
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0827c79fe1abb0348d5ed4b4df745b8a
https://doi.org/10.1002/chin.200323143
https://doi.org/10.1002/chin.200323143