Zobrazeno 1 - 10
of 40
pro vyhledávání: '"Maw Graham Nigel"'
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
Autor:
Andrews Mark David, Robert M. Owen, Mathilde Grenie, Kevin Beaumont, David C. Pryde, Sebastien Galan, Dannielle Frances Roberts, Tram T. Tran, Paul Alan Glossop, Amy S. Kenyon, Graham Lunn, Alan S. Jessiman, Maw Graham Nigel, Kerry af Forselles
Publikováno v:
ACS Medicinal Chemistry Letters. 6:419-424
The transient receptor potential (TRP) family of ion channels comprises nonselective cation channels that respond to a wide range of chemical and thermal stimuli. TRPM8, a member of the melastatin subfamily, is activated by cold temperatures (
SCOPE OF THE CHROMIUM(II)-MEDIATED SYNTHESIS OF E-ALKENYLSTANNANES FROM ALDEHYDES AND BU(3)SNCHBR(2)
The synthesis of E-alkenylstannanes from aldehydes and a mixture of Bu3SnCHBr2, LiI and CrCl2 is described. A mechanism is proposed to account for the alkene geometry in chromium(II)-mediated alkene synthesis which involves stereoselective addition b
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4db17364d269a97fcbd3a4957f3916da
https://doi.org/10.1016/0040-4020(95)00086-n
https://doi.org/10.1016/0040-4020(95)00086-n
Autor:
Charlotte Alice Louise Lane, David Ellis, Rachel Russel, Mathias John Paul, Lesa Watson, James R. Gosset, David James Rawson, Maw Graham Nigel, Street Stephen Derek Albert, Martin Corless, Mark E. Bunnage, Stephen Martin Denton, Kevin Beaumont, Laura Foster, Susan Cole, Stephen Ballard, Marion Floc’h, Jenny Price, William A. Million, Barber Christopher Gordon, Cedric Poinsard, David Leahy, Laura Barker, Frances Holmwood
Publikováno v:
Bioorganic & Medicinal Chemistry. 20:498-509
This paper describes our recent efforts to design and synthesise potent and selective PDE5 inhibitors and the use of in vitro predictors of clearance, absorption and permeability to maximise the potential for dose-proportional pharmacokinetics and go
Autor:
Emilio F. Stuart, Stuart Rozze, Fiona Macintyre, D. K. Walker, Michael A. Trevethick, Sandra Marina Monaghan, Michael Yeadon, Maw Graham Nigel, Patricia Wright, Simon John Mantell, Matthew D. Selby, Helene Chavaroche, Peter T. Stephenson, Arnaud Lemaitre, David V. Batchelor, Karen N. Wright, Lynsey Whitlock
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:4471-4475
COPD is a major cause of mortality in the western world. A(2A) agonists are postulated to reduce the lung inflammation that causes COPD. The cardiovascular effects of A(2A) agonists dictate that a compound needs to be delivered by inhalation to be th
Autor:
William A. Million, Pauline Carnell, Gareth W. Harbottle, Russell Monhemius, Simon A. Osborne, Cedric Poinsard, Maw Graham Nigel, Ben S. Greener, Karl Richard Gibson, Rebecca L. Prime, Steven England, Peter G. Dodd, Simon John Mantell, Alison Betts, Huw Rees
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:2190-2194
The SAR of a series of novel pyrido[3,4-d]pyramid-4-ylamine mGluR1 antagonists is described. The multiple of the unbound K(i) in cerebrospinal fluid necessary to give morphine like analgesic effects in an electromyograph pinch model in rodents is det
Autor:
Steven M. Gaulier, Dafydd R. Owen, Margarita Rodriguez-Lens, Huw Rees, Valerie A. Horne, Blanda Luzia Christa Stammen, Martin Corless, Maw Graham Nigel, Thomas Ryckmans, David W. Pearce, Ross A. Kinloch, Tracy J. Ringer
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:1702-1706
A number of libraries were produced to explore the potential of 2,4-diaminopyridine lead 1. The resulting diaminopyridines proved to be potent and selective delta-opioid receptor agonists. Several rounds of lead optimisation using library chemistry i
Autor:
D. K. Walker, Emilio F. Stuart, Arnaud Lemaitre, David V. Batchelor, Peter G. Dodd, Maw Graham Nigel, Helene Chavaroche, Sandra Marina Monaghan, Ruth F. Keir, Matthew D. Selby, Simon John Mantell, Tim J. Hobson, Michael A. Trevethick, Peter T. Stephenson, Stuart Rozze, Rhys M. Jones, Karen N. Wright, Michael Yeadon
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:1284-1287
COPD is a major cause of mortality in the western world. A(2A) agonists are postulated to reduce the lung inflammation that causes COPD. The cardiovascular effects of A(2A) agonists dictate that a compound needs to be delivered by inhalation to be th
Autor:
Gareth W. Harbottle, Maw Graham Nigel, Cedric Poinsard, Simon A. Osborne, Neil Feeder, Karl Richard Gibson, Mel Glossop, Florence F. Morel, William A. Million
Publikováno v:
Tetrahedron Letters. 48:4293-4296
The syntheses of 6-fluoropyrido[3,4-d]pyrimidin-4-ylamine derivatives is reported herein. Methods for generating C, N and O linked analogues under microwave irradiation are described.
Autor:
Simon Gayton, Graham Smith, Dafydd R. Owen, Gareth W. Harbottle, Tracy J. Ringer, Maw Graham Nigel, Simon A. Osborne, Margarita Rodriguez-Lens, Huw Rees, Peter G. Dodd, Ben S. Greener, Simon John Mantell
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:486-490
A series of novel mGluR1 antagonists have been prepared. Incorporation of fragments derived from weak lead matter into a library led to enhanced potency in a new chemical series. A chemistry driven second library iteration, covering a greatly enhance