Zobrazeno 1 - 10 of 43 pro vyhledávání: '"John E. Souness"'
1
An Algorithm-Directed Two-Component Library Synthesized Via Solid-Phase Methodology Yielding Potent and Orally Bioavailable p38 MAP Kinase Inhibitors
Autor: Kenneth Page, Stephen D. Pickett, Frank Halley, Iain Mcfarlane Mclay, Jeffrey Mckenna, John E. Souness, Collis Alan John, Imtiaz Ahmed
Publikováno v: Journal of Medicinal Chemistry. 45:2173-2184
Previously we reported the identification of RPR200765A, a potent orally bioavailable pyridine-imidazole inhibitor of p38 mitogen-activated protein (MAP) kinase which suppressed paw swelling and joint pathology in streptococcal cell wall-induced arth
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::38ba95ec4cb6eccd8facec065a16cf23
https://doi.org/10.1021/jm011132l
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3
Orally active indole N-oxide PDE4 inhibitors
Autor: Stevan W. Djuric, Rose Mathew, Richard Labaudiniere, Paul Joseph Cox, John E. Souness, Ken M. Page, Joanne Uhl, Bruce Miller, Christopher Hulme, Fu Chih Huang, Mercy Ramanjulu, Kevin J. Moriarty, Jeffrey Travis
Publikováno v: Bioorganic & Medicinal Chemistry Letters. 8:3053-3058
This communication describes the synthesis and in vitro and in vivo evaluation of a novel potent series of phosphodiesterase type (IV) (PDE4) inhibitors. Several of the compounds presented possess low nanomolar IC50's for PDE4 inhibition and excellen
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6cfa39770c13424996daf7b71d8543a0
https://doi.org/10.1016/s0960-894x(98)00572-1
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4
2-Substituted-4-methoxybenzimidazole-based PDE4 inhibitors
Autor: Hanney Barbara A, John E. Souness, Dennis Sweeney, Stevan W. Djuric, Joseph G. Bruno, Mcgarry Daniel G, Poli Gregory B, Jeffrey Travis, John R. Regan, Shelly Bower, Bruce Miller
Publikováno v: Bioorganic & Medicinal Chemistry Letters. 8:2737-2742
A new family of PDE4 inhibitors based on a benzimidazole framework is described. Several of these compounds are orally bioavailable and show efficacy in in vivo models of inflammatory disease.
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a2beaabedc332df64bc43591df5605a2
https://doi.org/10.1016/s0960-894x(98)00497-1
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5
Quaternary substituted PDE4 inhibitors I: The synthesis and in vitro evaluation of a novel series of oxindoles
Autor: John E. Souness, Fu Chih Huang, Christopher Hulme, Poli Gregory B, Stevan W. Djuric
Publikováno v: Bioorganic & Medicinal Chemistry Letters. 8:175-178
The following letter presents the synthesis and in vitro evaluation of a novel quaternary substituted series of phosphodiesterase type (IV) (PDE4) inhibitors. The compounds represent conformationally constrained analogues of the Celltech PDE IV inhib
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::06f17aa99573edc496143b65c04dc790
https://doi.org/10.1016/s0960-894x(97)10206-2
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6
Evidence that cyclic AMP phosphodiesterase inhibitors suppress interleukin-2 release from murine splenocytes by interacting with a ‘low-affinity’ phosphodiesterase 4 conformer
Autor: Clare Houghton, John E. Souness, Nughat Sardar, Withnall Michael Thomas
Publikováno v: British Journal of Pharmacology. 121:743-750
We have investigated the suppressive effects of rolipram, RP 73401 (piclamilast) and other structurally diverse inhibitors of cyclic AMP-specific phosphodiesterase 4 (PDE4) on interleukin (IL)-2 generation from Balb/c mouse splenocytes exposed to the
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::5a2b2af8d4a68d374c244a04b5b924b6
https://doi.org/10.1038/sj.bjp.0701200
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7
Evidence that cyclic AMP phosphodiesterase inhibitors suppress TNFα generation from human monocytes by interacting with a ‘low-affinity’ phosphodiesterase 4 conformer
Autor: Christopher Maslen, Miriam Griffin, Lisa C. Scott, John E. Souness, Jan-Anders Karlsson, Palfreyman Malcolm Norman, Kenneth Pollock, Karen Ebsworth
Publikováno v: British Journal of Pharmacology. 118:649-658
1. We have investigated the inhibitory effects of RP 73401 (piclamilast) and rolipram against human monocyte cyclic AMP-specific phosphodiesterase (PDE4) in relation to their effects on prostaglandin (PG)E2-induced cyclic AMP accumulation and lipopol
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::eb6409929e0c0b2cde6cde4160bb77ab
https://doi.org/10.1111/j.1476-5381.1996.tb15450.x
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8
Selective Type IV Phosphodiesterase Inhibitors as Antiasthmatic Agents. The Syntheses and Biological Activities of 3-(Cyclopentyloxy)-4-methoxybenzamides and Analogs
Autor: Ashton Michael John, Palfreyman Malcolm Norman, Andrew J. Ratcliffe, Sukanthini Thurairatnam, Nigel Vicker, Garry Fenton, Jan-Anders Karlsson, David Raeburn, John E. Souness, Cook David Charles
Publikováno v: Journal of Medicinal Chemistry. 37:1696-1703
The syntheses and biological activities of a number of benzamide derivatives, designed from rolipram, which are selective inhibitors of cyclic AMP-specific phosphodiesterase (PDE IV), are described. The effects of changes to the alkoxy groups, amide
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::57479afd583ea25fa89eabda2a79b8a8
https://doi.org/10.1021/jm00037a021
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9
Possible role of cyclic AMP phosphodiesterases in the actions of ibudilast on eosinophil thromboxane generation and airways smooth muscle tone
Autor: John E. Souness, Lisa C. Scott, David Raeburn, Mark A. Giembycz, Adrian Tomkinson, Maria Elena Villamil
Publikováno v: British Journal of Pharmacology. 111:1081-1088
1. The possible role of cyclic AMP phosphodiesterase (PDE) in the inhibitory actions of ibudilast on tracheal smooth muscle contractility and eosinophil thromboxane generation was investigated. 2. Ibudilast was a non-selective inhibitor of partially
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::734b0ccd9f5ba7c11f4070c9b4ffdad8
https://doi.org/10.1111/j.1476-5381.1994.tb14855.x
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