Zobrazeno 1 - 10
of 31
pro vyhledávání: '"J.S. Pillar"'
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
Publikováno v:
Journal of Biological Chemistry. 273:15559-15564
We have cloned and characterized the first human isozyme in a new family of cyclic nucleotide phosphodiesterases, PDE9A. By sequence homology in the catalytic domain, PDE9A is almost equidistant from all eight known mammalian PDE families but is most
Autor:
Peter F. Moore, A. Nagahisa, Saul B. Kadin, Francis J. Sweeney, Thomas J. Carty, P. P. Pazoles, M. J. Ernest, J. D. Cheng, J.S. Pillar, Leland D. Loose, P. A. Joseph, R. J. Griffiths, S. Murase, James D. Eskra
Publikováno v:
Inflammation Research. 46:168-179
Objective and Design: The effect of tenidap on the metabolism of arachidonic acid via the 5-lipoxygenase (5-LO) pathway was investigated in vitro and in vivo.¶Materials and Treatment: In vitro (cells). Arachidonic acid (AA) stimulated rat basophilic
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.
Publikováno v:
Journal of Labelled Compounds and Radiopharmaceuticals. 34:1147-1156
The 125I analog of MK-0591, 1, has been prepared for use as a radioligand for developing a 5-lipoxygenase activating protein (FLAP) binding assay. The radiosynthesis involves a two step oxidative iododestannylation-saponification procedure. A FLAP bi
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).
Autor:
G.W. Antognoli, C. Mebus, T.C. Liston, David B. Damon, R. J. Chambers, J. W. Watson, J.T. Shirley, A. Marfat, John B. Cheng, J.S. Pillar, Alexander V. Kuperman
Publikováno v:
Bioorganicmedicinal chemistry letters. 9(18)
CP-199,330 (3) and CP-199,331 (4) are cysLT1 receptor antagonists that are equipotent to marketed cysLT1 receptor antagonists zafirlukast and pranlukast, show good pharmacokinetics in rats and monkeys, and are devoid of liver toxicity in monkeys as s
Autor:
R. J. Chambers, Brian S. Owens, G.W. Antognoli, T.C. Liston, J.S. Pillar, Anthony Marfat, J.T. Shirley, John B. Cheng, Alexander V. Kuperman, John W. Watson
Publikováno v:
Bioorganicmedicinal chemistry letters. 8(24)
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).