Zobrazeno 1 - 10
of 32
pro vyhledávání: '"LTD4 receptor"'
Autor:
John G. Ball, Vincent Graffeo, Dianne K. Anestis, Gary O. Rankin, Suk K. Hong, Monica A. Valentovic
Publikováno v:
Toxicology. 300:92-99
The agricultural fungicide N-(3,5-dichlorophenyl)succinimide (NDPS) can induce marked nephrotoxicity in rats following a single intraperitoneal (ip) administration of 0.4 mmol/kg or greater. Although NDPS induces direct renal proximal tubular toxicit
Autor:
J. Scott Sawyer, Sandra L. Cockerham, K. Jeff Thrasher, Larry L. Froelich, Carlos R. Roman, Bach Nicholas J, Peter W. Stengel, Jerome H. Fleisch, Steven A. Silbaugh
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 6:249-252
A series of quinoline-substituted dihydroindoles has been synthesized and evaluated as antagonists of the cysLT 1 receptor. This series, exemplified by 2 (LY302905; pKi = 8.3 for inhibition of binding of 3 H-LTD 4 to guinea pig lung membranes), repre
Autor:
Marc Labelle, Paul J. Reider, Jacques Yves Gauthier, Paul Davis, Robert D. Larsen, Edward G. Corley, James D. Carroll, Xiang Yi Bin, Robert Zamboni, Anthony O. King, Thomas R. Verhoeven
Publikováno v:
The Journal of Organic Chemistry. 61:3398-3405
A general approach to the synthesis of a new class of LTD4 antagonists is presented. The key diarylpropane framework was prepared by Claisen−Schmidt condensation and selective reduction of the enone. Depending on the bridge to the 7-chloroquinaldin
Autor:
C. Rochette, Robert Zamboni, Anthony W. Ford-Hutchinson, Claude Dufresne, Marc Labelle, Deborah Slipetz, C. S. Mcfarlane, Thomas R. Jones, Yves Gareau, Lau Cheuk-Kun, Robert N. Young, L. Charette, Kathleen M. Metters, M. McAuliffe, Nicole Sawyer
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 5:1615-1620
Replacement of the quinoline pharmacophore of verlukast by alkylthiazoles and benzothiazoles has lead to the discovery of a new series of potent and orally active LTD4 receptor antagonists. The synthesis and structure activity relationships of this s
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:
E. G. ANDREWS, G. W. ANTOGNOLI, R. BRESLOW, M. P. CARTA, T. J. CARTY, R. J. CHAMBERS, J. B. CHENG, V. L. COHAN, J. L. COLLINS, D. B. DAMON, J. DELEHUNT, J. F. EGGLER, J. D. ESKRA, K. W. FREIERT, W. A. HADA, A. MARFAT, H. MASAMUNE, L. S. MELVIN, C. J. MULARSKI, B. A. NACLERIO, et al. et al.
Publikováno v:
ChemInform. 26
Autor:
Thomas R. Verhoeven, Anthony O. King, Paul J. Reider, Paul Davis, Edward G. Corley, James D. Carroll, Xiang Yi Bin, Marc Labelle, Robert Zamboni, Jacques Yves Gauthier, Robert D. Larsen
Publikováno v:
ChemInform. 27
A general approach to the synthesis of a new class of LTD4 antagonists is presented. The key diarylpropane framework was prepared by Claisen−Schmidt condensation and selective reduction of the enone. Depending on the bridge to the 7-chloroquinaldin
Autor:
David K. Herron, Bollinger Ng, Baldwin Rf, Jason Scott Sawyer, Carlos R. Roman, Richard Waltz Harper, L E Rinkema, Jerome H. Fleisch
Publikováno v:
Journal of Medicinal Chemistry. 35:1191-1200
A hypothetical model for receptor binding of leukotriene D4 (LTD4) was deduced from conformational analysis of LTD4 and from the structure-activity relationships (SAR) of known LTD4 receptor antagonists. A new structural series of LTD4 receptor antag
Publikováno v:
Journal of Labelled Compounds and Radiopharmaceuticals. 28:297-306
The synthesis of 5-[3-{2-(7-chloroquinolin-2-yl)ethenyl}-phenyl]-8-dimethylcarbamyl-4,6-[6-35S]dithiaoctanoic acid at a specific activity of 1350 Ci/mmol is reported. This compound is a reagent suited for selective affinity binding studies at the LTD