Zobrazeno 1 - 10
of 33
pro vyhledávání: '"J.T. Shirley"'
Autor:
John B. Cheng, Ajith V. Kamath, Douglas A. Fisher, Kelvin Lam, R. J. Chambers, Joann D. Pillar, Tessa A. Castleberry, Kristin Abrams, David Nettleton, John P. Umland, J.T. Shirley, C R Turner, Anthony Marfat, Alissa L. Sheils, E. D. Salter
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:718-721
Nicotinamide (2) is a potent and selective inhibitor of the PDE4D isozyme and as a chemical tool selectively blocks eosinophil mediator release and chemotaxis thus linking the role of PDE4D to eosinophil function.
Autor:
Molly A. McGlynn, Matthew Frank Brown, Stacie P. O'Sullivan, Anthony Marfat, John B. Cheng, Theodore E. Liston, John W. Watson, J.S. Pillar, David B. Damon, J.T. Shirley, R. J. Chambers, Gerard Antognoli, Brian S. Owens
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 8:2451-2456
Exploration of the indole nitrogen region of Zafirlukast (1) has uncovered a potent series of cysteinyl leukotriene D4 (LTD4) antagonists. These studies showed that a variety of functionality could be incorporated in this region of the molecule witho
Autor:
John P. Umland, Anthony Marfat, James F. Eggier, Sally C. Marshall, J.T. Shirley, Enrique Vazquez, Kelvin Cooper, Jeanene E. Tickner, Hiroko Masamune, John B. Cheng
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 5:1965-1968
The synthesis and the in vitro properties of a novel series of potent and selective phosphodiesterase type IV (PDE IV) inhibitors is described. Despite bearing structural similarity to rolipram, several of these compounds have much reduced affinity f
Autor:
Kelvin Cooper, Anthony Marfat, Jeenene E. Tickner, James F. Eggler, Hiroko Masamune, Allen J. Duplantier, Sally C. Marshall, John B. Cheng, Kenneth G. Kraus, John P. Umland, J.T. Shirley
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 5:1969-1972
The synthesis and biological properties of a novel series of potent and selective phosphodiesterase type IV (PDE IV) inhibitors are described. These catechol benzimidazoles were designed from rolipram and initial compounds reflected a similarly high
Autor:
Lawrence S. Melvin, Jeanene E. Tickner, John B. Cheng, J.T. Shirley, Frank W. Rusek, Anthony Marfat, James F. Eggler, Hiroko Masamune
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 5:1371-1376
A series of pyridine chromanols were synthesized and evaluated as LTD 4 -antagonists (LTD 4 -A). The quinoline sidechain of this class of such agents, as exemplified by REV-5901, has until now been deemed as essential for potent activity. However, by
Autor:
G.W. Antognoli, J.T. Shirley, A. Marfat, C.F. Wright, Thomas J. Carty, Frank W. Rusek, J. W. Watson, J. Delehunt, B. A. Naclerio, James F. Eggler, J.S. Pillar, Herbert Sherman, E.G. Andrews, Francis J. Sweeney, K. W. Freiert, R. Breslow, C. J. Mularski, V. L. Cohan, C J Pazoles, Lawrence S. Melvin, L.A. Rappach, John B. Cheng, David B. Damon, Jeanene E. Tickner, Judith L. Collins, P. Reiche, Hiroko Masamune, M. P. Carta, James D. Eskra, Hada William Andrew, R. J. Chambers
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 5:1365-1370
The development of two novel LTD 4 receptor antagonists as clinical candidates for the treatment of asthma is described. The first generation compound, CP-80,798, was found to be a balanced 5-lipoxygenase inhibitor (5-LOI)/LTD 4 antagonist (LTD 4 -A)
Autor:
Hiroko Masamune, J.T. Shirley, A. Marfat, John B. Cheng, Henry J. Showell, James F. Eggler, J.S. Pillar, Maryrose J. Conklyn, Jeanene E. Tickner, Lawrence S. Melvin, R. Breslow
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 5:887-892
The development of novel LTB 4 antagonists from a class of quinolylmethyl LTD 4 antagonists is described. These α-methyl quinolylmethyl chromanols were found to have good vitro activity.
Autor:
E. R. Pettipher, Allen J. Duplantier, K. L. Johnson, Kenneth G. Kraus, R. J. Chambers, T. A. Hibbs, John B. Cheng, Anthony Marfat, E. D. Salter, John P. Umland, T. H. Jenkinson, J.T. Shirley, V. L. Cohan, David B. Damon
Publikováno v:
ChemInform. 28
Tumor necrosis factor-α (TNF-α) has been implicated as a key mediator in the progression of rheumatoid arthritis. Inhibitors of phosphodiesterase IV (PDE IV) have been shown to inhibit the production of TNF-α by elevating intracellular levels of c
Autor:
John W. Watson, Anthony Marfat, John B. Cheng, J.T. Shirley, R. J. Chambers, G.W. Antognoli, J.S. Pillar
Publikováno v:
ChemInform. 29
By addressing the issues of potency and metabolism in 3, a new series of LTD4 antagonists represented by (+)-26 was developed which is equipotent to clinical LTD4 antagonists Zafirlukast (1) and Pranlukast (2).
Autor:
T.C. Liston, Anthony Marfat, G.W. Antognoli, John B. Cheng, J.S. Pillar, Alexander V. Kuperman, J.T. Shirley, R. J. Chambers, Brian S. Owens, John W. Watson
Publikováno v:
ChemInform. 30
A new series of cysLT1 receptor antagonists represented by CP-288,886 (7) and CP-265,298 (8) were developed which are equipotent to clinical cysLT1 receptor antagonists Zafirlukast (1) and Pranlukast (2).