Zobrazeno 1 - 5
of 5
pro vyhledávání: '"Ward John Gerard"'
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:
Ward John Gerard, Macpherson David T, Stuart Bailey, Pearl Louis-Flamberg, Lisa Marshall, Ruth J. Mayer, David Smith, Mistry Jayshree, Peter Henry Milner, Brian Bolognese, Andrew Faller
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 9:3165-3170
Using a variety of alpha-hydroxy hydroxamic acid derivatives, the size and shape of the S1' pocket for the CD23 processing metalloprotease has been explored. It has been demonstrated that a P1' 2-naphthylmethyl group occupies most of the available sp
Autor:
Alan Naylor, R. Dunsdon, A. O'Brien, Rosalie Matico, Paul Rowland, Daryl S. Walter, Sharon Sweitzer, P. Theobald, Peter Henry Milner, Sally Redshaw, Gareth Wayne, G. Maile, B. Clarke, D. Vesey, David MacPherson, Emmanuel Hubert Demont, Kathrine J. Smith, J. Mosley, Andrew Faller, Ishrut Hussain, Ward John Gerard, Virginie Soleil, Julie Hawkins, Steven J. Stanway, Geoffrey Stemp, Colin Dingwall, David R. Riddell
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(3)
This paper describes the discovery of non-peptidic, potent, and selective hydroxy ethylamine (HEA) inhibitors of BACE-1 by replacement of the prime side of a lead di-amide 2 . Inhibitors with nanosmolar potency and high selectivity were identified. D
Autor:
Steven J. Stanway, Alistair Stuart, John Skidmore, Sally Redshaw, Rosalie Matico, Geoffrey Stemp, Paul Rowland, A. O'Brien, Daryl S. Walter, Nicolas Charrier, Christopher N. Johnson, David R. Riddell, Peter Henry Milner, Sharon Sweitzer, Kathrine J. Smith, Gareth Wayne, Alan Naylor, Paul John Beswick, Colin Dingwall, Ward John Gerard, Julie Hawkins, J. Mosley, David MacPherson, P. Theobald, Emmanuel Hubert Demont, D. Vesey, Andrew Faller, G. Maile, Virginie Soleil, Robert Gleave, R. Dunsdon, Ishrut Hussain, B. Clarke
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(3)
This article is focusing on further optimization of previously described hydroxy ethylamine (HEA) BACE-1 inhibitors obtained from a focused library with the support of X-ray crystallography. Optimization of the non-prime side of our inhibitors and in
Autor:
Paul Rowland, J. Mosley, Sally Redshaw, Ishrut Hussain, Peter Henry Milner, Rosalie Matico, Gareth Wayne, Colin Dingwall, Andrew Faller, Geoffrey Stemp, Emmanuel Hubert Demont, Kathrine J. Smith, P. Theobald, David MacPherson, B. Clarke, G. Maile, R. Dunsdon, David R. Riddell, Alan Naylor, Daryl S. Walter, Julie Hawkins, D. Vesey, Virginie Soleil, A. O'Brien, Sharon Sweitzer, Steven J. Stanway, Ward John Gerard
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(3)
Inhibition of the aspartyl protease BACE-1 has the potential to deliver a disease-modifying therapy for Alzheimer’s disease. Herein, is described the lead generation effort which resulted, with the support of X-ray crystallography, in the discovery