Zobrazeno 1 - 10
of 16
pro vyhledávání: '"Jay DaRe"'
Autor:
Jay DaRe, Qun Dang, Mark D. Erion, Tony Gibson, Frank Taplin, Paul D. van Poelje, Yan Liu, Scott C. Potter, Srinivras Rao Kasibhatla, K. Raja Reddy, Wei Xiao, Gerard R. Scarlato
Publikováno v:
Journal of Medicinal Chemistry. 53:441-451
Efforts to enhance the inhibitory potency of the initial purine series of fructose-1,6-bisphosphatase (FBPase) inhibitors led to the discovery of a series of benzimidazole analogues with human FBPase IC(50)s < 100 nM. Inhibitor 4.4 emerged as a lead
Autor:
and Juergen M. Schanzer, James B. Wiesner, Jay DaRe, Joseph J. Kopcho, Mark D. Erion, Angelo J. Castellino, Bheemarao G. Ugarkar
Publikováno v:
Journal of Medicinal Chemistry. 43:2883-2893
Adenosine receptor agonists produce a wide variety of therapeutically useful pharmacologies. However, to date they have failed to undergo successful clinical development due to dose-limiting side effects. Adenosine kinase inhibitors (AKIs) represent
Autor:
Ross Dixon, Mark D. Erion, James R. Appleman, Jay DaRe, James M. Fujitaki, Angelo J. Castellino, James B. Wiesner, Bheemarao G. Ugarkar
Publikováno v:
Nucleosides and Nucleotides. 16:1013-1021
The pyrrolopyrimidine nucleoside GP3269 (12) was shown to be a potent and selective inhibitor of human adenosine kinase (IC50 = 11 nM) and to exhibit anticonvulsant activity in rats after oral administration. Synthesis of GP3269 was accomplished in 4
Autor:
Jay DaRe, Tao Jiang, Scott C. Potter, Tony Gibson, Qun Dang, Frank Taplin, Yan Liu, Mark D. Erion, Daniel K. Cashion, Haiqing Li, Zhili Sun, Jason D. Jacintho, Paul D. van Poelje, Srinivas Rao Kasibhatla, Yi Fan, Lemus Robert Huerta, Feng Tian, Wenyu Li
Publikováno v:
Journal of medicinal chemistry. 54(1)
Oral delivery of previously disclosed purine and benzimidazole fructose-1,6-bisphosphatase (FBPase) inhibitors via prodrugs failed, which was likely due to their high molecular weight (>600). Therefore, a smaller scaffold was desired, and a series of
Autor:
James M. Fujitaki, Angelo J. Castellino, Ross Dixon, Mark D. Erion, James R. Appleman, James B. Wiesner, Bheemarao G. Ugarkar, Jay DaRe
Publikováno v:
ChemInform. 29
The pyrrolopyrimidine nucleoside GP3269 (12) was shown to be a potent and selective inhibitor of human adenosine kinase (IC50 = 11 nM) and to exhibit anticonvulsant activity in rats after oral administration. Synthesis of GP3269 was accomplished in 4
Autor:
Jay DaRe, Serge H. Boyer, Timothy J. Colby, Paul D. van Poelje, Mark D. Erion, Kristin Ollis, William Craigo, Zhili Sun, Michael C Matelich, Jorge E. Gomez-Galeno, James M. Fujitaki, K. Raja Reddy, Bheemarao G Ugarkar
Publikováno v:
Journal of medicinal chemistry. 51(3)
Adefovir dipivoxil, a marketed drug for the treatment of hepatitis B, is dosed at submaximally efficacious doses because of renal toxicity. In an effort to improve the therapeutic index of adefovir, 1-aryl-1,3-propanyl prodrugs were synthesized with
Publikováno v:
Nucleosides and Nucleotides. 9:649-662
Ribavirin and tiazofurin, two nucleosides of known antiviral activity, have been transformed by previously reported methods to yield several deoxy,epoxy, or dideoxy analogues. The deoxygenated derivatives were evaluated for antiviral activity against
Publikováno v:
Neuroscience letters. 220(2)
The adenosine kinase inhibitor, 5'-deoxyiodotubercidin (5dITU), was examined in a rat focal stoke model with temporary (105 min) middle cerebral artery occlusion (MCAO) followed by a 24 h recovery period. Inhibition of this adenosine metabolizing enz
Autor:
Michael A. Ussery, Bjarne Gabrielsen, Melinda G. Hollingshead, John W. Huggins, Bheema Ugarkar, Michael J. Phelan, Jay DaRe, William M. Shannon, Ernst M. Schubert, Thomas P. Monath, Grazyna Groszek, Jorma J. Kirsi, George R. Pettit, Deborah F. Kefauver
Publikováno v:
Journal of natural products. 55(11)
A series of 23 Amaryllidaceae isoquinoline alkaloids and related synthetic analogues were isolated or synthesized and subsequently evaluated in cell culture against the RNA-containing flaviviruses (Japanese encephalitis, yellow fever, and dengue viru
Autor:
Qun Dang, Yan Liu, Daniel K. Cashion, Srinivas Rao Kasibhatla, Tao Jiang, Frank Taplin, Jason D. Jacintho, Haiqing Li, Zhili Sun, Yi Fan, Jay DaRe, Feng Tian, Wenyu Li, Tony Gibson, Robert Lemus, Paul D. van Poelje, Scott C. Potter, Mark D. Erion
Publikováno v:
Journal of Medicinal Chemistry; Jan2011, Vol. 54 Issue 1, p153-165, 13p