Zobrazeno 1 - 10
of 23
pro vyhledávání: '"Russell A. Lewthwaite"'
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:
Valerie A. Ashwood, Christine Julien-Larose, Lakhbir Singh, Russell Andrew Lewthwaite, Scott McCleary, Mark J. Field, Jenny Raphy, M.C. Pritchard, David C. Horwell
Publikováno v:
Journal of Medicinal Chemistry. 44:2276-2285
This paper describes the synthesis and physical and biological effects of introducing different substituents at the alpha-position of the tryptophan containing neurokinin-1 receptor antagonist [(R)-2-(1H-indol-3-yl)-1-methyl-1-((S)-1-phenyl-ethylcarb
Autor:
N. Suman-Chauhan, Alexander T. McKnight, John Hughes, David C. Horwell, Valerie A. Ashwood, Russell Andrew Lewthwaite, V. Brownhill, M. Higginbottom, C. Webb, Steven Williams, M.C. Pritchard, R. D. Pinnock
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 8:2589-2594
In this paper we describe the development of a novel series of non-peptide, "balanced" neuromedin-B preferring (BB1)/gastrin-releasing peptide preferring (BB2) receptor ligands as exemplified by PD 176252. PD 176252, which exhibits nanomolar affinity
Autor:
J. Ronald Rubin, Russell A. Lewthwaite, David C. Horwell, Martyn Clive Pritchard, Ratcliffe Giles S
Publikováno v:
Tetrahedron. 54:4591-4606
A series of piperazinone ring systems have been synthesised as a means of evaluating the effect of conformational restriction on high affinity non-peptide NK1, NK3 and CCK-B receptor ligands. The synthesis of the targeted heterocycles is described al
Autor:
Russell Andrew Lewthwaite, R. E. Jordan, J. C. O'toole, M.C. Pritchard, N. Suman-Chauhan, W. Howson, Steven Williams, Alexander T. McKnight, K. Martin, John Hughes, M. Higginbottom, Rob D. Pinnock, J. M. Eden, M. D. Hall, David C. Horwell
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 6:2617-2622
In this paper we describe the development of a novel series of non-peptide neuromedin-B (NMB) receptor ligands as exemplified by PD 165929. PD 165929, which exhibits nanomolar affinity for the NMB receptor (Ki=6.3nM), has been demonstrated to be a co
Publikováno v:
Liquid Crystals. 16:299-313
This article describes how the inclusion and positioning of a lateral hydroxy group influences the thermal stability of a chiral smectic C phase. An off-central position of the hydroxy group in the aromatic core has the effect of enhancing the therma
Autor:
Robert T. Smith, Jane L. Burrows, Arnaud Lemaitre, Samantha Hughes, Peter G. Dodd, Tim J. Evans, Russell Andrew Lewthwaite, Mathias John Paul, Mark H. Stefaniak, Michael Yeadon, James Philip, David S. Millan, Mark E. Bunnage, Christopher Phillips, Kenneth John Butcher, Iain Kilty, David Fairman, Axel Mahnke
Publikováno v:
Journal of medicinal chemistry. 54(22)
This paper describes the identification and optimization of a novel series of DFG-out binding p38 inhibitors as inhaled agents for the treatment of chronic obstructive pulmonary disease. Structure based drug design and "inhalation by design" principl
Autor:
Anne Phelan, Iain Kilty, Russell Andrew Lewthwaite, Darren Baldock, David S. Millan, Mathias John Paul, Frank Stuhmeier, David G. Brown, Andrew Pannifer, Samantha Hughes, Mark Anthony O'reilly
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(21)
We report the use of fragment screening and fragment based drug design to develop a PI3γ kinase fragment hit into a lead. Initial fragment hits were discovered by high concentration biochemical screening, followed by a round of virtual screening to
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:
N. Suman-Chauhan, M.C. Pritchard, R. E. Jordan, John Hughes, Alexander T. McKnight, Rob D. Pinnock, Russell Andrew Lewthwaite, J. C. O'toole, David C. Horwell, M. Higginbottom, Steven Williams, J. M. Eden, K. Martin, M. D. Hall, W. Howson
Publikováno v:
ChemInform. 28
In this paper we describe the development of a novel series of non-peptide neuromedin-B (NMB) receptor ligands as exemplified by PD 165929. PD 165929, which exhibits nanomolar affinity for the NMB receptor (Ki=6.3nM), has been demonstrated to be a co