Zobrazeno 1 - 9
of 9
pro vyhledávání: '"James B. Coutcher"'
Autor:
William H. Martin, Banavara L. Mylari, Peter J. Oates, James B. Coutcher, Michael C. Linhares, David A. Tess, Michael S. Dina, David A. Beebe, Gregory J. Withbroe, Sandra J Armento, Melissa O'Gorman, William James Zembrowski, Edward L. Conn
Publikováno v:
Journal of Medicinal Chemistry. 48:6326-6339
Discovery of a highly selective, potent, and safe non-carboxylic acid, non-hydantoin inhibitor of aldose reductase (AR) capable of potently blocking the excess glucose flux through the polyol pathway that prevails under diabetic conditions has been a
Autor:
Peter J. Oates, Jian-Cheng Li, David A. Beebe, R. Matthew Weekly, Day Wesley Warren, Margaret Y. Chu-Moyer, William E. Ballinger, James B. Coutcher
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 12:1477-1480
SAR studies on the stereoisomers of CP-470,711 suggested that in vivo epimerization was taking place in rats. Further metabolism studies revealed that no epimerization was occurring in dogs, and that no epimerization was expected in humans. A mechani
Autor:
Michael S. Dina, Nathaniel S. Brackett, Peter J. Oates, James B. Coutcher, William James Zembrowski, Banavara L. Mylari, David A. Beebe
Publikováno v:
ChemInform. 32
We report here on our medicinal chemistry and pharmacology efforts to provide a potent sorbitol dehydrogenase inhibitor (SDI) as a tool to probe a recently disclosed hypothesis centered on the role of sorbitol dehydrogenase (SDH) in the second step o
Publikováno v:
Diabetes. 55(10)
Previously studied inhibitors of aldose reductase were largely from two chemical classes, spirosuccinamide/hydantoins and carboxylic acids. Each class has its own drawbacks regarding selectivity, in vivo potency, and human safety; as a result, the pa
Autor:
David A. Beebe, James B. Coutcher, William James Zembrowski, Banavara L. Mylari, Peter J. Oates, Gregory J. Withbroe, Edward L. Conn, Nathaniel S. Brackett
Publikováno v:
Bioorganicmedicinal chemistry. 11(19)
Two new templates, (R) 2-hydroxyethyl-pyridine and (R) 2-hydroxyethyl-triazine, were used to design novel sorbitol dehydrogenase inhibitors (SDIs). The design concept included spawning of these templates to function as effective ligands to the cataly
Autor:
James B. Coutcher, Gregory J. Withbroe, Peter J. Oates, Melissa O'Gorman, Michael S. Dina, Edward L. Conn, William H. Martin, Banavara L. Mylari, William James Zembrowski, David A. Tess, David A. Beebe, Sandra J Armento, Michael C. Linhares
Publikováno v:
Journal of medicinal chemistry. 46(12)
We report here on the discovery path that led to a structurally unprecedented non-hydantoin, non-carboxylic acid aldose reductase inhibitor, 24, which shows remarkably potent oral activity in normalizing elevated sorbitol levels and, more significant
Autor:
Peter J. Oates, Michael C. Linhares, Gregory J. Withbroe, James B. Coutcher, Edward L. Conn, William James Zembrowski, Melissa O'Gorman, Banavara L. Mylari, David A. Beebe
Publikováno v:
Journal of medicinal chemistry. 45(20)
We report here a novel sorbitol dehydrogenase inhibitor, 16, that shows very high oral potency (50 microg/kg) in normalizing elevated fructose levels in the sciatic nerve of chronically diabetic rats and sustained duration of action (24 h). Furthermo
Autor:
Day Wesley Warren, David A. Beebe, Margaret Y. Chu-Moyer, William E. Ballinger, Peter J. Oates, Banavara L. Mylari, Jiancheng Li, James B. Coutcher, Richard Berger, R. Matthew Weekly
Publikováno v:
Journal of medicinal chemistry. 45(2)
Optimization of a previously disclosed sorbitol dehydrogenase inhibitor (SDI, II) for potency and duration of action was achieved by replacing the metabolically labile N,N-dimethylsulfamoyl group with a variety of heterocycles. Specifically, this eff
Autor:
Banavara L. Mylari, Peter J. Oates, Michael S. Dina, David A. Beebe, James B. Coutcher, Nathaniel S. Brackett, William James Zembrowski
Publikováno v:
Journal of medicinal chemistry. 44(17)
We report here on our medicinal chemistry and pharmacology efforts to provide a potent sorbitol dehydrogenase inhibitor (SDI) as a tool to probe a recently disclosed hypothesis centered on the role of sorbitol dehydrogenase (SDH) in the second step o