Zobrazeno 1 - 10
of 36
pro vyhledávání: '"G. Maile"'
Autor:
Alan Naylor, Emmanuel Hubert Demont, P. Theobald, Daryl S. Walter, G. Maile, Gareth Wayne, Ishrut Hussain, Colin Dingwall, B. Clarke, C. Howes, Sharon Sweitzer, D. Vesey, Leanne Cutler, Julie Hawkins, Rosalie Matico, J. Mosley, A. O'Brien, Virginie Soleil, Sally Redshaw, Kathrine J. Smith, Paul Rowland, R. Dunsdon
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:4639-4644
Inhibition of the aspartyl protease BACE-1 has the potential to deliver a disease-modifying therapy for Alzheimer's disease. Herein, is described a series of potent inhibitors based on an hydroxyethylamine (HEA) transition state mimetic template. The
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::851f861c6b32aae4d35275a238821e3a
https://doi.org/10.1016/j.bmcl.2010.05.111
https://doi.org/10.1016/j.bmcl.2010.05.111
Autor:
D. Vesey, B. Clarke, Sharon Sweitzer, Julie Hawkins, A. O'Brien, Alan Naylor, J. Mosley, Nicolas Charrier, Julia A. Hubbard, G. Maile, Ishrut Hussain, Virginie Soleil, Paul Rowland, Kathrine J. Smith, Rosalie Matico, Colin Dingwall, Daryl S. Walter, R. Dunsdon, Gareth Wayne, P. Theobald, Emmanuel Hubert Demont, Sally Redshaw
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:3669-3673
Our first generation of hydroxyethylamine transition-state mimetic BACE-1 inhibitors allowed us to validate BACE-1 as a key target for Alzheimer's disease by demonstrating amyloid lowering in an animal model, albeit at rather high doses. Finding a mo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6c26f979a9c8455e33fb53f47794d028
https://doi.org/10.1016/j.bmcl.2009.03.150
https://doi.org/10.1016/j.bmcl.2009.03.150
Autor:
D. Vesey, Daryl S. Walter, Nicolas Charrier, G. Maile, Emmanuel Hubert Demont, P. Theobald, Sally Redshaw, A. O'Brien, R. Dunsdon, Alan Naylor
Publikováno v:
Synthesis. 2006:3467-3477
Traditional strategies in indole chemistry do not allow high-yielding access to some substitution patterns such as 3,5,7-trisubstituted indoles. We report in this article the efficient synthesis of this type of indole. The Heck cyclisation strategy w
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::068428ef4603016ca1c6229df9ac9c9f
https://doi.org/10.1055/s-2006-950223
https://doi.org/10.1055/s-2006-950223
Autor:
G. Maile, P. Theobald, Nicolas Charrier, Alan Naylor, R. Dunsdon, Daryl S. Walter, A. O'Brien, D. Vesey, Emmanuel Hubert Demont, Sally Redshaw
Publikováno v:
Synlett. :3071-3074
Traditional strategies in indole chemistry do not allow high yielding access to some substitution patterns such as 3,5,7-trisubstituted indoles. We report in this article the efficient synthesis of this type of indole. The Heck cyclisation strategy w
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::95062aaf316965556e06717750f22f37
https://doi.org/10.1055/s-2005-921917
https://doi.org/10.1055/s-2005-921917
Publikováno v:
Journal of Labelled Compounds and Radiopharmaceuticals. 44:149-164
The development of the collagenase inhibitor, cipemastat (Ro 32-3555), required the synthesis of both carbon-14 labelled and deuteriated material for the measurement of the parent drug and drug-related material in biological fluids. In addition, labe
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::7540a226518c1c0484d13f50a9d47f8a
https://doi.org/10.1002/jlcr.440
https://doi.org/10.1002/jlcr.440
Autor:
Ishrut Hussain, G. Maile, A. O'Brien, Gareth Wayne, Julie Hawkins, Daryl S. Walter, Sharon Sweitzer, Virginie Soleil, B. Clarke, P. Theobald, Colin Dingwall, Emmanuel Hubert Demont, Alan Naylor, Paul Rowland, Rosalie Matico, Kathrine J. Smith, Leanne Cutler, J. Mosley, C. Howes, Sally Redshaw, R. Dunsdon, Julia A. Hubbard, Nicolas Charrier, D. Vesey
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(13)
Our first generation of hydroxyethylamine BACE-1 inhibitors proved unlikely to provide molecules that would lower amyloid in an animal model at low oral doses. This observation led us to the discovery of a second generation of inhibitors having nanom
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::836066c48bc0736fb08b7d4a29c3cf6e
https://pubmed.ncbi.nlm.nih.gov/19406640
https://pubmed.ncbi.nlm.nih.gov/19406640
Autor:
B. Clarke, Paul Rowland, Sharon Sweitzer, D. Vesey, G. Maile, Rosalie Matico, Virginie Soleil, A. O'Brien, Sally Redshaw, Daryl S. Walter, Nicolas Charrier, Alan Naylor, J. Mosley, Julie Hawkins, Gareth Wayne, Emmanuel Hubert Demont, R. Dunsdon, Leanne Cutler, Kathrine J. Smith, P. Theobald, Julia A. Hubbard, Colin Dingwall, C. Howes, Ishrut Hussain
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(13)
Inhibition of the aspartyl protease BACE-1 has the potential to deliver a disease-modifying therapy for Alzheimer's disease. We have recently disclosed a series of transition-state mimetic BACE-1 inhibitors showing nanomolar potency in cell-based ass
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a0f1ad6694ef3d789a072ff208cb01b2
https://pubmed.ncbi.nlm.nih.gov/19428244
https://pubmed.ncbi.nlm.nih.gov/19428244
Autor:
D. Vesey, Alan Naylor, Rosalie Matico, P. Jeffrey, Daryl S. Walter, Nicolas Charrier, Julie Hawkins, Sharon Sweitzer, B. Clarke, Paul Rowland, Ishrut Hussain, R. Dunsdon, A. O'Brien, Philip East, Colin Dingwall, Virginie Soleil, J. Mosley, Emmanuel Hubert Demont, Leanne Cutler, Sally Redshaw, Kathrine J. Smith, C. Howes, P. Theobald, G. Maile, Gareth Wayne
Publikováno v:
Journal of medicinal chemistry. 51(11)
BACE-1 inhibition has the potential to provide a disease-modifying therapy for the treatment of Alzheimer’s disease. Optimization of a first generation of BACE-1 inhibitors led to the discovery of novel hydroxyethylamines (HEAs) bearing a tricyclic
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3bba0eace56f44a64342f037ce8c9dae
https://pubmed.ncbi.nlm.nih.gov/18457381
https://pubmed.ncbi.nlm.nih.gov/18457381
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bf4cc2f54e1e1fb8b7f62e700d29eba9
https://pubmed.ncbi.nlm.nih.gov/18166458
https://pubmed.ncbi.nlm.nih.gov/18166458
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::002bb92212c2a4d3edcd6c86b819b2d5
https://pubmed.ncbi.nlm.nih.gov/18171615
https://pubmed.ncbi.nlm.nih.gov/18171615