Zobrazeno 1 - 10
of 55
pro vyhledávání: '"George W, Koszalka"'
Publikováno v:
Clinical Pharmacology in Drug Development.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::777b95f5f367c0f5dc7dce4b9bca743c
https://doi.org/10.1002/cpdd.1217
https://doi.org/10.1002/cpdd.1217
Autor:
George W. Koszalka, Kamalesh P. Ruppa, Polina Lyuboslavsky, David S. Menaldino, Raymond Dingledine, Dennis C. Liotta, Stephen F. Traynelis, Zackery W. Dentmon, Lawrence J. Wilson, Scott J. Myers, Robert Zaczek, Yesim Altas Tahirovic
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 379:41-52
We describe a clinical candidate molecule from a new series of glutamate N-methyl-d-aspartate receptor subunit 2B-selective inhibitors that shows enhanced inhibition at extracellular acidic pH values relative to physiologic pH. This property should r
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::f0c1e8e93e3ee0c58291395f09218349
https://doi.org/10.1124/jpet.120.000370
https://doi.org/10.1124/jpet.120.000370
Autor:
Zongjian Zhu, George W. Koszalka, Dennis C. Liotta, Rhonda L. Moore, Steven A. Kell, David S. Menaldino, Stephen F. Traynelis, Scott J. Myers, Samantha L. Summer
Publikováno v:
ACS Medicinal Chemistry Letters. 10:248-254
[Image: see text] The N-methyl-d-aspartate receptor plays a critical role in central nervous system processes. Its diverse properties, as well as hypothesized role in neurological disease, render NMDA receptors a target of interest for the developmen
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2c559418bdd69a66568a49ad1830a0f2
https://doi.org/10.1021/acsmedchemlett.8b00395
https://doi.org/10.1021/acsmedchemlett.8b00395
Autor:
Scott J, Myers, Kamalesh P, Ruppa, Lawrence J, Wilson, Yesim A, Tahirovic, Polina, Lyuboslavsky, David S, Menaldino, Zackery W, Dentmon, George W, Koszalka, Robert, Zaczek, Raymond J, Dingledine, Stephen F, Traynelis, Dennis C, Liotta
Publikováno v:
J Pharmacol Exp Ther
We describe a clinical candidate molecule from a new series of glutamate N-methyl-d-aspartate receptor subunit 2B–selective inhibitors that shows enhanced inhibition at extracellular acidic pH values relative to physiologic pH. This property should
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::db965d485c48ecef3089d635d22d3940
https://pubmed.ncbi.nlm.nih.gov/34493631
https://pubmed.ncbi.nlm.nih.gov/34493631
Autor:
Lloyd Frick, John C. Drach, Joseph H. Chan, Dean W. Selleseth, Stanley D. Chamberlain, George W. Koszalka, Ernest H. Dark, Robert J. Harvey, Karen K. Biron, Leroy B. Townsend, R E Dornsife, Michelle G. Davis
Publikováno v:
Nucleosides, Nucleotides and Nucleic Acids. 19:101-123
A series of 2'-deoxy analogues of the antiviral agent 5,6-dichloro-2-isopropylamino-1-(beta-L-ribofuranosyl)-1H-benzimidazole (1263W94) were synthesized and evaluated for activity against human cytomegalovirus (HCMV) and for cytotoxicity. The 2-subst
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::75e3c56352778834b481dfb60df98d2e
https://doi.org/10.1080/15257770008032999
https://doi.org/10.1080/15257770008032999
Autor:
Ruiming Zou, Etsuko Kawashima, Leroy B. Townsend, John C. Drach, George Andrew Freeman, George W. Koszalka
Publikováno v:
Nucleosides, Nucleotides and Nucleic Acids. 19:125-153
Stereoselective glycosylation of 2,5,6-trichlorobenzimidazole (1b), 2-bromo-5,6-dichlorobenzimidazole (1c), 5,6-dichlorobenzimidazole (1d), 5,6-dichlorobenzimidazole-2-thione (1e), 5,6-dichloro-2-(methylthio)benzimidazole (1f), 2-(benzylthio)-5,6-dic
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9f1c38fc12f18fd8acaa8e32097c9730
https://doi.org/10.1080/15257770008033000
https://doi.org/10.1080/15257770008033000
Autor:
Michael T. Migawa, John C. Drach, Jean-Luc Girardet, Stanley D. Chamberlain, George W. Koszalka, John A. Walker, Leroy B. Townsend
Publikováno v:
Journal of Medicinal Chemistry. 41:1242-1251
Several 2-substituted alpha-D- and alpha-L-lyxofuranosyl and 5-deoxylyxofuranosyl derivatives of 5,6-dicholro-2-(isopropylamino)-1-(beta-L-ribofuranosyl) benzimidazole (1263W94) and 2,5,6-trichloro-1(beta-D-ribofuranosyl)benzimidazole (TCRB) were syn
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a92c1124c19c20cbd2613b841d1edb31
https://doi.org/10.1021/jm970545c
https://doi.org/10.1021/jm970545c
Autor:
Thomas A. Krenitsky, Steven E. Ealick, William J. Cook, Min Zhou, Chen Mao, George W. Koszalka
Publikováno v:
Structure. 5(10):1373-1383
Background: Purine nucleoside phosphorylase (PNP) from Escherichia coli is a hexameric enzyme that catalyzes the reversible phosphorolysis of 6-amino and 6-oxopurine (2′-deoxy)ribonucleosides to the free base and (2′-deoxy)ribose-1-phosphate. In
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::38f97d8cc08cd74e8bf51f15aec35b42
Autor:
George Andrew Freeman, G. Szczech, George W. Koszalka, Steven A. Short, N. A. Van Draanen, Robert J. Harvey, Robert Jansen
Publikováno v:
Journal of Medicinal Chemistry. 39:538-542
A series of 2'-deoxy-4'-thioribo purine nucleosides was prepared by trans-N-deoxyribosylase-catalyzed reaction of 2'-deoxy-4'-thiouridine with a variety of purine bases. This synthetic procedure is an improvement over methods previously used to prepa
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8275ede2160624424a4572e6d631e0d4
https://doi.org/10.1021/jm950701k
https://doi.org/10.1021/jm950701k
Publikováno v:
Nucleosides and Nucleotides. 13:1679-1693
A series of α-L-2′,3′-dideoxy nucleosides was prepared as potential antiviral agents. The pyrimidine nucleosides were prepared by standard Vorbruggen coupling reactions. The purine analogues were prepared by enzymatic transfer of the dideoxy sug
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::0344afeae8dbedcad768328f415d0f35
https://doi.org/10.1080/15257779408009473
https://doi.org/10.1080/15257779408009473