Zobrazeno 1 - 10
of 12
pro vyhledávání: '"Charlotte Alice Louise Lane"'
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:
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:
David Howard Williams, Nigel Alan Swain, Charlotte Alice Louise Lane, Michael Paradowski, Duncan Hay, Matthew D. Selby, Charles E. Mowbray
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:1156-1159
This letter describes the discovery and synthesis of a series of octahydropyrrolo[3,4-c]pyrrole based selective histamine hH4 receptor antagonists. The amidine compound 20 was found to be a potent and selective histamine H4 receptor antagonist with m
Publikováno v:
Synlett. 2011:1543-1546
A concise synthesis of fused bicyclic pyrrolidines via 1,3-dipolar cycloaddition of azomethine ylides is reported. The exo cycloadduct isomer enables the synthesis of a novel cyclic amidine toward the preparation of a potential human histamine H4 rec
Autor:
Charlotte Alice Louise Lane, Mike Trevethick, Russell Andrew Lewthwaite, Kim James, Christelle Perros-Huguet, Mark E. Bunnage, Rhys M. Jones, Paul Alan Glossop, David Price, Rob Webster, Simon John Mantell, Alan Daniel Brown
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:4012-4015
The design and profile of a series of saligenin containing long acting β2-adrenoreceptor agonists is described. Evaluation of these analogues using a guinea-pig tissue model demonstrates that analogues within this series have significantly longer du
Autor:
Barber Christopher Gordon, David James Rawson, Maw Graham Nigel, Natalie M. Mount, David G. Brown, Charlotte Moira Norfor Allerton, Susan M. Cole, Charlotte Alice Louise Lane, David Ellis, Nicholas W. Summerhill, Colin Robinson, Kevin Beaumont, Street Stephen Derek Albert
Publikováno v:
Journal of Medicinal Chemistry. 49:3581-3594
Sildenafil (5-[2-ethoxy-5-(4-methyl-1-piperazinylsulfonyl)phenyl]-1-methyl-3-n-propyl-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one), a potent and selective phosphodiesterase type 5 (PDE5) inhibitor, provided the first oral treatment for male erectil
Autor:
Francesca Perrucio, M. Abid Masood, Graham Smith, Charles E. Mowbray, M. J. Gardner, Helen Kenyon-Edwards, Charlotte Alice Louise Lane, Rhys M. Jones, Andrew Simon Bell, Wai L. Liu, Andrew C. Mansfield, Matthew D. Selby, Nick Clarke, Christopher D. Brown, Rachel Osborne
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(21)
We describe the identification of a potent, selective lead series that shows antagonism against the human histamine H4 receptor from thirteen actives identified in an HTS as part of a hit to lead program. By focusing on ligand efficiency and concurre
Autor:
Emanuel Schenck, Wai L. Liu, Rhys M. Jones, Nick Clarke, Charlotte Alice Louise Lane, Michael Paradowski, Charles E. Mowbray, Michelle Collins, Mathew D. Selby, Andrew Simon Bell, David Howard Williams, Sandra D. Newman, Nigel Alan Swain
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(21)
We describe the development of novel benzimidazoles as small molecule histamine H4 receptor (H4R) antagonists and their profiling in rat early toxicity studies. The discovery and optimisation of a second series of pyrimidine based antagonists is then
Autor:
Mark E. Bunnage, Neil Feeder, Jane L. Burrows, Russell Andrew Lewthwaite, Fiona J. Spence, Paul Alan Glossop, Rob Webster, Charlotte Alice Louise Lane, Nick Clarke, Michael A. Trevethick, Alan Daniel Brown, Kim James, David Price, Christelle Perros-Huguet, Michael Yeadon, Stefan Colin John Taylor, Rhys M. Jones
Publikováno v:
Journal of medicinal chemistry. 53(18)
A novel series of potent and selective sulfonamide derived β(2)-adrenoreceptor agonists are described that exhibit potential as inhaled ultra-long-acting bronchodilators for the treatment of asthma and chronic obstructive pulmonary disease. Analogue
Autor:
Christelle Perros-Huguet, Rob Webster, Mark E. Bunnage, Paul Alan Glossop, Rhys M. Jones, David Price, Simon John Mantell, Mike Trevethick, Russell Andrew Lewthwaite, Kim James, Alan Daniel Brown, Charlotte Alice Louise Lane
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(4)
The design and profile of a series of adamantyl-containing long acting β 2 -adrenoreceptor agonists are described. An optimal pharmacokinetic profile of low oral bioavailability was combined with a strong pharmacology profile when assessed using a g