Zobrazeno 1 - 10
of 30
pro vyhledávání: '"Mark G. Vartanian"'
Autor:
Brian Nichelson, Mark G. Vartanian, Charles Taylor, Susan M. Lotarski, Nancy Sue Barta, Sean D. Donevan, Sian E. Gibbons, Norman L. Colbry, Zhu Zhijian, Melvin R. Dickerson, Paul Galatsis, Russell J. DeOrazio, Jacob Bradley Schwarz, Kristin Knapp Lin, Zheng Li, Andrew John Thorpe, Jack J. Kinsora, Raymond Andrew Hudack, David J. Wustrow, David D. Manning, Ayman El-Kattan
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:3559-3563
Several beta-amino tetrazole analogs of gabapentin 1 and pregabalin 2 were prepared by one of two convergent, highly efficient routes, and their affinity for the alpha(2)-delta protein examined. Two select compounds with potent affinity for alpha(2)-
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e71639ec10a452e24f369e2dc36c1c1f
https://doi.org/10.1016/j.bmcl.2006.03.083
https://doi.org/10.1016/j.bmcl.2006.03.083
Autor:
Jack J. Kinsora, N. Suman-Chauhan, Clare O. Kneen, Karen Walters, Cindy M. Donovan, David J. Wustrow, Thomas Capiris, David J. Dooley, Ayman El-Kattan, Mark G. Vartanian, Lisa R. Thompson, Susan M. Lotarski, Simon A. Osborne, Jacob Bradley Schwarz, Mark J. Field, Carmen E. Burgos-Lepley, Charles Taylor, Justin Stephen Bryans, Madhu Cherukury
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:2333-2336
A series of carboxylate bioisosteres of structures related to gabapentin 1 have been prepared. When the carboxylate was replaced by a tetrazole, this group was recognized by the alpha2-delta protein. Further characterization of alpha2-delta binding c
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::15c268505093a43a39031f57a037129d
https://doi.org/10.1016/j.bmcl.2005.05.016
https://doi.org/10.1016/j.bmcl.2005.05.016
Autor:
Louis L. Radulovic, Mark G. Vartanian, Jack J. Kinsora, Edward H. Bertram, Charles Taylor, Kevin A. Serpa, M. Vergnes
Publikováno v:
Epilepsy Research. 68:189-205
Pregabalin (Lyrica) is a novel amino acid compound that binds with high affinity to the alpha2-delta (alpha2-delta) auxiliary protein of voltage-gated calcium channels. In vivo, it potently prevents seizures, pain-related behaviors and has anxiolytic
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::296da83529c9c68836624a40449cd41e
https://doi.org/10.1016/j.eplepsyres.2005.11.001
https://doi.org/10.1016/j.eplepsyres.2005.11.001
Autor:
Thomas G. Heffner, Jack J. Kinsora, Jacob Bradley Schwarz, Ti Zhi-Su, David J. Wustrow, Leonard T. Meltzer, Thomas Richard Belliotti, Thomas Capiris, Andrew John Thorpe, Lawrence D. Wise, Mark L. Weber, Charles Taylor, Mark J. Field, Mark G. Vartanian, I.Victor Ekhato
Publikováno v:
Journal of Medicinal Chemistry. 48:2294-2307
Pregabalin exhibits robust activity in preclinical assays indicative of potential antiepileptic, anxiolytic, and antihyperalgesic clinical efficacy. It binds with high affinity to the alpha(2)-delta subunit of voltage-gated calcium channels and is a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c05d681e9f725c4f7d0de7f09212832b
https://doi.org/10.1021/jm049762l
https://doi.org/10.1021/jm049762l
Autor:
Charles Taylor, Kadee J. Raser, Avigail Posner, John J. Cordon, Kevin K.W. Wang, Nancy C. Kupina, Gerald P. Schielke, Mark G. Vartanian
Publikováno v:
Developmental Brain Research. 95:169-175
This study was performed to investigate whether the anticonvulsant phenytoin has neuroprotective effect in a model of hypoxia-ischemia with neonatal rats. The left carotid artery of each rat was ligated, followed by 3 h of hypoxic exposure (8% O2) in
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::59a1d84614dfd418b600448726953bea
https://doi.org/10.1016/0165-3806(96)00073-9
https://doi.org/10.1016/0165-3806(96)00073-9
Autor:
Daniel F. Ortwine, Peter A. Boxer, Leonard Joseph Lescosky, S. A. Borosky, Daniel Martin Retz, C.B. Nelson, Thomas Charles Malone, Christopher F. Bigge, Mark G. Vartanian, Schelkun Robert Michael
Publikováno v:
Journal of Medicinal Chemistry. 38:3720-3740
Four related series of substituted quinoxalinediones containing angular fused-piperidine rings have been synthesized as α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonists with potential as neuroprotective agents, primar
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ebe1f78653faecd9283d29ff86e0bbd8
https://doi.org/10.1021/jm00019a003
https://doi.org/10.1021/jm00019a003
Autor:
Christopher F. Bigge, Jia-He Li, Susan A. Borosky, Rufus M. Williamson, Daniel F. Ortwine, Mark G. Vartanian
Publikováno v:
Journal of Medicinal Chemistry. 38:1955-1965
A series of enantiomerically pure (phosphonomethyl)-substituted phenylalanine derivatives related to SDZ EAB 515 (1) were prepared as competitive N-methyl-D-aspartate (NMDA) receptor antagonists. Unlike most known competitive NMDA antagonists, analog
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f09fa37f51b06607d4543f8a0603d7df
https://doi.org/10.1021/jm00011a015
https://doi.org/10.1021/jm00011a015
Autor:
P. A. Boxer, Roy D. Schwarz, Mark G. Vartanian, Sheryl J. Hays, Michael J. Rice, Daniel F. Ortwine, Denise K. Boyd, Graham Johnson, Laura F. Copeland
Publikováno v:
Journal of Pharmaceutical Sciences. 83:1425-1432
Thirty-two aryl-substituted 2-benzothiazolamines have been tested for their ability to modulate sodium flux in rat cortical slices. A QSAR analysis, applied to these derivatives, showed a trend toward increasing potency as sodium flux inhibitors with
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ce799d3690e3f0f1e904d41795d3f2d4
https://doi.org/10.1002/jps.2600831013
https://doi.org/10.1002/jps.2600831013
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 4:823-826
PD144723, S-(+)-3-isobutyl GABA, is structurally related to both the inhibitory neurotransmitter γ-aminobutyric acid and the novel anticonvulsant gabapentin. That the S-enantiomer is more potent than the R-(-)-enantiomer, PD144550, for in vitro disp
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::7d6f9c496bf454535c453f16fff22447
https://doi.org/10.1016/s0960-894x(01)80855-6
https://doi.org/10.1016/s0960-894x(01)80855-6
Publikováno v:
Epilepsy Research. 16:175-181
The concentration-time profile of [14C]gabapentin (GBP) in plasma and brain interstitial fluid (ISF) was determined following a single 15 mg/kg intravenous bolus dose to rats. Brain ISF was sampled with a microdialysis probe in striatum. Blood was al
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f7cf72b47c8a1a17087b238508a3c65c
https://doi.org/10.1016/0920-1211(93)90078-l
https://doi.org/10.1016/0920-1211(93)90078-l