Zobrazeno 1 - 10
of 12
pro vyhledávání: '"Alan, Macinnes"'
Autor:
Brian R. Bond, D. Joseph Rogier, Yi Zheng, Maddux Todd Michael, Sharon Lu, Alan MacInnes, Jeanne M. Rumsey, John K. Walker, E. Jon Jacobsen, Robert Hughes, Seungil Han
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:6348-6352
We describe the design, synthesis and profiling of a novel series of PDE5 inhibitors. We take advantage of an alternate projection into the solvent region to identify compounds with excellent potency, selectivity and pharmacokinetic profiles.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5fa3656b2c0c95aea695fd40890798ca
https://doi.org/10.1016/j.bmcl.2011.08.106
https://doi.org/10.1016/j.bmcl.2011.08.106
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[
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::892c7788c8aa398973abd4f8bb5a78a5
https://doi.org/10.1021/jm901781q
https://doi.org/10.1021/jm901781q
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5005db6742e606fdadbf520ea66a63a9
https://doi.org/10.1016/j.bmcl.2009.06.012
https://doi.org/10.1016/j.bmcl.2009.06.012
Publikováno v:
Diabetes. 55:1855-1861
Glycogen phosphorylase inhibition represents a promising strategy to suppress inappropriate hepatic glucose output, while muscle glycogen is a major source of fuel during contraction. Glycogen phosphorylase inhibitors (GPi) currently being investigat
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4626d5e8df06e096a2cbf32f11b2fa07
https://doi.org/10.2337/db05-1687
https://doi.org/10.2337/db05-1687
Autor:
James A. Timmons, Alan MacInnes
Publikováno v:
Current Research in Animal Physiology
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::67c415f0a775626c0baf6ff03b0b944e
https://doi.org/10.1201/b12225-7
https://doi.org/10.1201/b12225-7
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[
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::88c2de53db53a1f8525bbef66ae6a7e3
https://pubmed.ncbi.nlm.nih.gov/20196613
https://pubmed.ncbi.nlm.nih.gov/20196613
Autor:
Craig L. Hyde, Maruja E. Lira, Sara A. Paciga, Alan MacInnes, Frances A. Sanders, Diederik F. van Wijk, Ole Faergeman, Richard Mazzarella, Linda S. Wood, John F. Thompson
Publikováno v:
Circulation. Cardiovascular genetics, 3(2), 162-168. Lippincott Williams and Wilkins
Hyde, C L, Macinnes, A, Sanders, F A, Thompson, J F, Mazzarella, R A, Faergeman, O, Vanwijk, D F, Wood, L, Lira, M & Paciga, S A 2010, ' Genetic Association of the CCR5 Region with Lipid Levels in At-Risk Cardiovascular Patients ', Circulation . https://doi.org/10.1161/CIRCGENETICS.109.897793
Hyde, C L, Macinnes, A, Sanders, F A, Thompson, J F, Mazzarella, R A, Faergeman, O, Vanwijk, D F, Wood, L, Lira, M & Paciga, S A 2010, ' Genetic Association of the CCR5 Region with Lipid Levels in At-Risk Cardiovascular Patients ', Circulation . https://doi.org/10.1161/CIRCGENETICS.109.897793
Background— There is mounting evidence to suggest that chemokine receptor 5 (CCR5) plays an important role in the development and progression of atherosclerosis. A naturally occurring variant of the CCR5 gene CCR532, exists at allele frequencies of
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::303c8c4afe76a116b285e5fcbddb3a38
https://pubmed.ncbi.nlm.nih.gov/20130232
https://pubmed.ncbi.nlm.nih.gov/20130232
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::56bba8721c0b4d57439e25992ba23e4b
https://pubmed.ncbi.nlm.nih.gov/19631533
https://pubmed.ncbi.nlm.nih.gov/19631533
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3c530b519c26bbcf215a387ac7749266
https://pubmed.ncbi.nlm.nih.gov/19539468
https://pubmed.ncbi.nlm.nih.gov/19539468
Autor:
Alan MacInnes, James A. Timmons
Publikováno v:
BMC Physiology, Vol 5, Iss 1, p 11 (2005)
BMC Physiology
BMC Physiology
Background Patients suffering from Intermittent Claudication (IC) experience repeated periods of muscle contraction with low blood flow, throughout the day and this may contribute to the hypothesised skeletal muscle abnormalities. However, no study h
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2c8ff7ac1324eb5236e8f170395e8ea2
https://doi.org/10.1186/1472-6793-5-11
https://doi.org/10.1186/1472-6793-5-11