Zobrazeno 1 - 8
of 8
pro vyhledávání: '"Lisa R. Thompson"'
Autor:
Mark L. Lewis, Charlotte Alice Louise Lane, Blanda Luzia Christa Stammen, David James Rawson, Peter J. Bungay, William A. Million, Stephen Martin Denton, Sharan K. Bagal, Tanya L. Hay, C. Elizabeth Payne, Lisa R. Thompson, Maw Graham Nigel, Cedric Poinsard, Karl Richard Gibson, Kemp Mark Ian, Edward B. Stevens, Melanie S. Glossop
Publikováno v:
ACS Medicinal Chemistry Letters. 6:650-654
Voltage-gated sodium channels, in particular Nav1.8, can be targeted for the treatment of neuropathic and inflammatory pain. Herein, we described the optimization of Nav1.8 modulator series to deliver subtype selective, state, and use-dependent chemi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::498d91e57ef91a319caeeab504bffe20
https://doi.org/10.1021/acsmedchemlett.5b00059
https://doi.org/10.1021/acsmedchemlett.5b00059
Autor:
Lisa R. Thompson, Dafydd R. Owen, Tim Young, Isabelle Tran, Martin Paul Edwards, Michelle F. Tutt, Ana Monica Correia, Val A. Horne, Thomas Ryckmans
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:4406-4409
A series of libraries were designed using the 1-(cyclopropylmethyl)-2-alkyl-4,5,6,7-tetrahydro-1 H -imidazo[4,5- c ]pyridin-5-ium templates 2a – b , and Sulfonamide derivatives 11a – n proved to be potent agonists of the CB 2 receptor. Analysis o
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::45612526872047a270414b7c175e3402
https://doi.org/10.1016/j.bmcl.2009.05.062
https://doi.org/10.1016/j.bmcl.2009.05.062
Autor:
Ian B. Moses, M. Jonathan Fray, Adam T. Gillmore, Keith A. Reeves, Lisa R. Thompson, Melanie S. Glossop, David J. McManus, Céline F. B. Praquin
Publikováno v:
Organic Process Research & Development. 14:263-271
The development is described of a viable kilo-scale synthesis of the Nav1.8 sodium channel modulator, N-methyl-6-amino-5-(2,3,5-trichlorophenyl)pyridine-2-carboxamide (PF-1247324) in five steps, starting from 6-amino-5-bromo-2-picoline, in 33% overal
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::a356863667163c037ec41c1cc47c6278
https://doi.org/10.1021/op900092h
https://doi.org/10.1021/op900092h
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:
David James Rawson, Delphine Brugier, Maw Graham Nigel, Paul Turnpenny, Jo Hough, Anthony Harrison, Julie Newman, Lisa R. Thompson, Jenny Price, Joe Otterburn, Andrew N. Warren
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(12)
A potent series of substituted (2 S ,4 S )-benzylproline α 2 δ ligands have been designed from the readily available starting material (2 S ,4 R )-hydroxy- l -proline. The ligands have improved pharmacokinetic profile over the (4 S )-phenoxyproline
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1efddf21d78fbc6a5973fd63565f1f96
https://pubmed.ncbi.nlm.nih.gov/21550802
https://pubmed.ncbi.nlm.nih.gov/21550802
Autor:
David James Rawson, David C. Blakemore, Andrew N. Warren, Justin Stephen Bryans, Wai-Lam Alexis Chu, Maw Graham Nigel, Delphine Brugier, Lisa R. Thompson, Cedric Poinsard
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(12)
A new series of glycine-derived ligands of the α(2)δ subunit of voltage gated calcium channels is described. Several novel compounds (7) based on (6) were prepared that possessed a potency
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bb091acad7f37c0d62b0024063a7ccfc
https://pubmed.ncbi.nlm.nih.gov/21601457
https://pubmed.ncbi.nlm.nih.gov/21601457
Autor:
Julie Newman, Maw Graham Nigel, Jo Hough, David James Rawson, Lisa R. Thompson, Anthony Harrison, Andrew N. Warren, Jenny Price, Delphine Brugier, Paul Turnpenny, Joe Otterburn
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(12)
Conformational constraint has been used to design a potent series of α(2)δ ligands derived from the readily available starting material (2S,4R)-hydroxy-l-proline. The ligands have improved physicochemistry and potency compared to their linear count
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5a2aa6ec29397c4db0f25d57a6d916e0
https://pubmed.ncbi.nlm.nih.gov/21550803
https://pubmed.ncbi.nlm.nih.gov/21550803
Autor:
Jack K. Kinsora, Lisa R. Thompson, Pauline Carnell, Mark J. Field, Natasha Kinsella, Justin Stephen Bryans, Sophie Caroline Williams, Simon A. Osborne, David C. Blakemore, Leonard T. Meltzer
Publikováno v:
ChemInform. 41
A range of 3,4-alkylated five-membered ring derivatives of gabapentin were synthesised. One compound (21) had an excellent level of potency against alpha(2)delta and was profiled in in vivo models of pain and anxiety.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::2c4faaf5604decc4e73dc9001e210902
https://doi.org/10.1002/chin.201021061
https://doi.org/10.1002/chin.201021061