Zobrazeno 1 - 10
of 27
pro vyhledávání: '"Emma J. Carlson"'
Autor:
Wai-Si Eng, Xinchun Tong, Richard Tschirret-Guth, Song Zheng, Gary G. Chicchi, Geoge A. Doss, Koppara Samuel, Richard Hargreaves, Terence G. Hamill, Marc M. Kurtz, Robert J. DeVita, Sanjeev Kumar, Alan Wheeldon, Emma J. Carlson, Alana Upthagrove, Jaime Lynn Bunda, Stephen Krause, Jinlong Jiang, Christine Ryan, Sander G. Mills, Donald Burns, Kwei-Lan C. Tsao
Publikováno v:
Journal of Medicinal Chemistry. 52:3039-3046
3-[(3aR,4R,5S,7aS)-5-{(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy}-4-(4-fluorophenyl)octahydro-2H-isoindol-2-yl]cyclopent-2-en-1-one (17) is a high affinity, brain-penetrant, hydroisoindoline-based neurokinin-1 (NK(1)) receptor antagonist with a lo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d21762545018b32ec2dc16a2b6444d66
https://doi.org/10.1021/jm8016514
https://doi.org/10.1021/jm8016514
Autor:
Peter Lin, Gary G. Chicchi, Julie A. DeMartino, Neil Collinson, Marc M. Kurtz, Susan Boyce, Robert J. DeVita, Alan Wheeldon, Jonathan R. Young, Stephen Moore, Emma J. Carlson, Kwei-Lan C. Tsao, Sander G. Mills, Karen Townson, George A. Doss, Gregori J. Morriello, Nadia M.J. Rupniak
Publikováno v:
Bioorganic & Medicinal Chemistry. 16:2156-2170
Previous work on human NK(1) antagonists in which the core of the structure is a substituted pyrrolidine has been disclosed. These compounds showed good binding affinity and functional IP activity, however, many did not exhibit the necessary brain pe
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a07bdec5af551942f4ff8d7149d7c129
https://doi.org/10.1016/j.bmc.2007.11.081
https://doi.org/10.1016/j.bmc.2007.11.081
Autor:
Janusz Jozef Kulagowski, Gary G. Chicchi, Clare London, Alan Wheeldon, Ian Thomas Huscroft, Emma J. Carlson, Marc M. Kurtz, Piotr Raubo
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:2008-2012
1-Phenyl-8-azabicyclo[3.2.1]octane ethers are NK1 receptor antagonists. Substitution at the 6-exo-position led to high affinity NK1 antagonists with a prolonged duration of action in vivo. Incorporation of an α-methyl substituent in the pendent benz
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e93157e3f9b3b77746bfe5a3bca6ab93
https://doi.org/10.1016/j.bmcl.2005.12.069
https://doi.org/10.1016/j.bmcl.2005.12.069
Autor:
Ruth O'Donnell, Smith David W, Susan Boyce, T. Harrison, Nadia M.J. Rupniak, Michael Rigby, Louise Hewson, Emma J. Carlson
Publikováno v:
Neuropharmacology. 41:130-137
The involvement of the basolateral amygdala in mediating the inhibition of neonatal vocalisation by substance P (NK(1) receptor) antagonists was examined. These studies determined whether the time course for separation-induced vocalisations in guinea
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ee3c8b8a88bc14f82aa1cafdf2f42093
https://doi.org/10.1016/s0028-3908(01)00051-x
https://doi.org/10.1016/s0028-3908(01)00051-x
Publikováno v:
Experimental Neurology. 155:49-58
NMDA-mediated neurotoxicity and oxidative stress have been implicated in the etiology of a number of degenerative diseases including motor neuron disease. The present study examined the effect of chronic administration of the glycine/NMDA receptor an
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::936444f1c41647ca88e55033284aad50
https://doi.org/10.1006/exnr.1998.6873
https://doi.org/10.1006/exnr.1998.6873
Autor:
Angela Williams, Raymond G. Hill, Guanghan Liu, Margaret A. Cascieri, John J. Sramek, John P. Feighner, Gary G. Chicchi, Ram K. Shrivastava, Malcolm MacCoss, Edward M. Scolnick, Duane B. Snavely, Emma J. Carlson, Louise Hewson, Christopher John Swain, Jeffrey J. Hale, Sharon Sadowski, N.R. Cutler, David D. Smith, Nadia M.J. Rupniak, Franz Hefti, Timothy Harrison, Edwina Wyatt-Knowles, Sander G. Mills, Scott A. Reines, Richard Hargreaves, John Carman, Mark S. Kramer
Publikováno v:
Science. 281:1640-1645
The localization of substance P in brain regions that coordinate stress responses and receive convergent monoaminergic innervation suggested that substance P antagonists might have psychotherapeutic properties. Like clinically used antidepressant and
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::888508e4bee9b37a82f2f5da6928e9e3
https://doi.org/10.1126/science.281.5383.1640
https://doi.org/10.1126/science.281.5383.1640
Autor:
Susan Boyce, Kwei-Lan Tsao, Gary G. Chicchi, Karen Townson, Sander G. Mills, Julie A. DeMartino, Neil Collinson, Marc M. Kurtz, Gregori J. Morriello, Robert J. DeVita, Alan Wheeldon, Nadia M.J. Rupniak, Emma J. Carlson, Tricia Johnson, Xinchun Tong, Song Zheng
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(19)
Previously, we had disclosed a novel class of hNK(1) antagonists based on the 5,5-fused pyrrolidine core. These compounds displayed subnanomolar hNK(1) affinity along with good efficacy in a gerbil foot-tapping (GFT) model, but unfortunately they had
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6a8e996df1a1b78f6c5cafc9b1d3ed98
https://pubmed.ncbi.nlm.nih.gov/20729082
https://pubmed.ncbi.nlm.nih.gov/20729082
Autor:
Gary G. Chicchi, Kwei-Lan C. Tsao, Huagang Lu, Xinchun Tong, Gregori J. Morriello, Robert J. DeVita, Alan Wheeldon, Emma J. Carlson, Sander G. Mills, Song Zheng, Jianming Bao, Marc M. Kurtz
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(7)
A new class of potent NK1 receptor antagonists with a tetrahydroindolizinone core has been identified. This series of compounds demonstrated improved functional activities as compared to previously identified 5,5-fused pyrrolidine lead structures. SA
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f528cd8177c783967c22911a6cf6d1ce
https://pubmed.ncbi.nlm.nih.gov/20188553
https://pubmed.ncbi.nlm.nih.gov/20188553
Autor:
Karen Townson, Gregori J. Morriello, Kwei-Lan Tsao, Gary G. Chicchi, Nadia M.J. Rupniak, Sander G. Mills, Mikhail Reibarkh, Philip Davies, Julie A. DeMartino, Neil Collinson, Alan Wheeldon, Marc M. Kurtz, Stephen Moore, Tricia Johnson, F.D. Tattersall, Susan Boyce, Robert J. DeVita, Emma J. Carlson, Song Zheng, Xinchun Tong
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(6)
Previous work on human NK(1) (hNK(1)) antagonists in which the core of the structure is a 5,5-fused pyrrolizinone has been disclosed. The structural-activity-relationship studies on simple alpha- and beta-substituted compounds of this series provided
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2c5f1466795a40ae5e39fb30c2992976
https://pubmed.ncbi.nlm.nih.gov/20153964
https://pubmed.ncbi.nlm.nih.gov/20153964
Autor:
Cherilyn Turner, Alan Wheeldon, Sander G. Mills, Gary G. Chicchi, Robert J. DeVita, Jonathan R. Young, Kwei-Lan C. Tsao, Emma J. Carlson, Marc M. Kurtz, Ronsar Eid
Publikováno v:
Bioorganicmedicinal chemistry letters. 17(19)
The preparation and structure-activity-relationships of novel pyrrolidine-carboxamides and oxadiazoles are described. Compounds in this series were found to be potent hNK(1) antagonists in vitro and efficacious in vivo with minimal interactions with
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ff751abca0250c4b312599844e5efbe8
https://pubmed.ncbi.nlm.nih.gov/17723300
https://pubmed.ncbi.nlm.nih.gov/17723300