Zobrazeno 1 - 10
of 81
pro vyhledávání: '"Mervyn Thompson"'
Autor:
David Thornhill, Charles McCartan, Ian George Mervyn Thompson, Stephen Spence, Jonathan Talbot-Weiss
Publikováno v:
SAE International Journal of Engines. 4:1354-1364
Autor:
Alison I. Muir, Izzy Boyfield, Kalindi Vaidya, Barry Sidney Orlek, Etienne Fleury, David G. Evans, Jackie S. Scott, Hindy Mok, Victoria J. Bolton, Ward John Gerard, Geoffrey Stemp, Tom D. Heightman, Kim L. Matthews, Kirk Lawless, Gareth J. Sanger, Fiona McKay, Alexander J. Stevens, Emma M. Jarvie, James Matthew Bailey, Susan Marie Westaway, Mervyn Thompson, Jonathan B. Basilla
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:6452-6458
Optimisation of a series of benzazepine sulfonamide hit compounds identified from high throughput screening led to the discovery of a new series of tractable, potent motilin receptor agonists.
Autor:
Kim Winborn, Sarah C. Lappin, James S. Wright, Vicky Holland, Martin J. Gunthorpe, Harshad Kantilal Rami, Andrew D. Randall, Sandra Arpino, Graham D Smith, Julie Egerton, Stephen J. Brough, Mervyn Thompson, Jeffrey C. Jerman, Sara Luis Hannan, Darren Smart, John B. Davis
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 321:1183-1192
Vanilloid receptor-1 (TRPV1) is a nonselective cation channel, predominantly expressed by sensory neurons, which plays a key role in the detection of noxious painful stimuli such as capsaicin, acid, and heat. TRPV1 antagonists may represent novel the
Autor:
Jeffrey C. Jerman, Darren Smart, Andrew D. Randall, Becky Sargent, Steve Fell, Geoffrey Stemp, Harshad Kantilal Rami, Alexander J. Stevens, Dominic Sanderson, Martin J. Gunthorpe, John B. Davis, Mervyn Thompson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:3287-3291
Small molecule antagonists of the vanilloid receptor TRPV1 (also known as VR1) are disclosed. Pyrrolidinyl ureas such as 8 and 15 (SB-705498) emerged as lead compounds following optimisation of the previously described urea SB-452533. Pharmacological
Autor:
Jenifer Powles, Neil Upton, Kim Winborn, Nigel Deeks, Christopher N. Johnson, Tania Buck, Mahmood Ahmed, Brenda K. Trail, Darren Jason Mitchell, Mervyn Thompson, Vicky Holland, Laurie J. Gordon, Michael A. Briggs, Jon T. Seal, Stephen Moss, Ashley Garner, David R. Witty, Steven Mark Bromidge, Lorraine Campbell, Andrew D. Medhurst, Tania O. Stean, Geoffrey Stemp, Dieter Hamprecht
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:4867-4871
Starting from the potent and selective but poorly brain penetrant 5-HT6 receptor antagonist SB-271046, a successful strategy for improving brain penetration was adopted involving conformational constraint with concomitant reduction in hydrogen bond c
Autor:
Mark S. Duxon, Peter J. Atkinson, Tracey E. Shaw, David R. Thomas, Kevin M. Thewlis, Michael S. Hadley, Beverley Hammond, Geoffrey Stemp, Gary W. Price, Claire M. Scott, Vong Antonio Kuok Keong, Jeannette M. Watson, Steven Mark Bromidge, Christopher N. Johnson, Graham J. Riley, Derek N. Middlemiss, Harshad Kantilal Rami, Stephanie E. North, Laramie Mary Gaster, Kathryn R. Starr, Mervyn Thompson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:737-741
Starting from a high throughput screening hit, a series of 3,4-dihydro-2H-benzoxazinones has been identified with both high affinity for the 5-HT(1A) receptor and potent 5-HT reuptake inhibitory activity. The 5-(2-methyl)quinolinyloxy derivative comb
Autor:
Michael J. Welsh, Mervyn Thompson, Antony Chadderton, Jennifer L. Leonard, Harshad Kantilal Rami, Qin J. Zhang, Laramie Mary Gaster, Karen A. Augustine-Rauch, Patrick J. Wier
Publikováno v:
Birth Defects Research Part A: Clinical and Molecular Teratology. 70:789-807
BACKGROUND SB-236057 is a potent skeletal teratogen in rodents and rabbits, producing axial and posterior somite malformations in cultured rat embryos. The compound shares some structural similarity to cyclopamine. METHODS M13 phage display was used
Autor:
S. Nasir, Angela Worby, Catherine H. Gill, Harshad Kantilal Rami, Wyman Paul Adrian, Jeffrey C. Jerman, Andrew D. Randall, John B. Davis, Mervyn Thompson, Darren Smart, Julie Egerton, Ellen M. Soffin, Davina E. Owen, Graham D Smith, Ceri H. Davies, Sarah C. Lappin, Martin J. Gunthorpe, L. Howett, S. Luis Hannan
Publikováno v:
Neuropharmacology. 46:133-149
Vanilloid receptor-1 (TRPV1) is a non-selective cation channel, predominantly expressed by peripheral sensory neurones, which is known to play a key role in the detection of noxious painful stimuli, such as capsaicin, acid and heat. To date, a number
Autor:
Joseph P. Adams, Paul R. Raithby, Catherine J. Smith, Stephen D. Roughley, Ian Thomson Forbes, Andrew B. Holmes, Martin E. Fox, Mervyn Thompson, Geoffrey M. Williams, John E. Davies, Edwin C. Davison, Neil John Press
Publikováno v:
Journal of the Chemical Society, Perkin Transactions 1. :1494-1514
An intramolecular hydroxylamine-alkyne cyclisation is used for the enantioselective synthesis of the cyclic nitrones 36 and 44. We have demonstrated the use of a novel nitrone protection strategy by cycloaddition of styrene to the cyclic nitrone 44 i
Publikováno v:
Synthetic Communications. 32:2555-2563
A simple procedure for the preparation of 1,7-disubstituted-1,2,3,4-tetrahydroisoquinolines from 3,4-dihydroisoquinoline (2) is presented. This strategy overcomes the limitation of cyclisation appr...