Zobrazeno 1 - 10
of 11
pro vyhledávání: '"Haydn, Beaton"'
Autor:
Karin Kaspersson, Ian Gurrell, Elisabeth Bäck, Samantha Budd Haeberlein, Karin Kolmodin, Roland Bürli, Michael J. McKenzie, Susanna Eketjäll, Philip Thorne, Patrik Johansson, Jörg Holenz, Gvido Cebers, Clay W Scott, Mark E. Duggan, Paul R. J. Davey, Haydn Beaton
Publikováno v:
Journal of medicinal chemistry. 61(8)
BACE1 is responsible for the first step in APP proteolysis, leading to toxic Aβ production, and has been indicated to play a key role in the pathogenesis of Alzheimer's disease. The related isoform BACE2 is thought to be involved in processing of th
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c2deb1ce7f84601bfeead883d644af7b
https://pubmed.ncbi.nlm.nih.gov/29617572
https://pubmed.ncbi.nlm.nih.gov/29617572
Autor:
Aaron Rigby, Peter J. H. Webborn, Rob Riley, John Collington, Mark Furber, Brian Springthorpe, Matt Soars, Ash Bahl, Cathy MacDonald, Keith Bowers, Elizabeth Kinchin, Lilian Alcaraz, Rebecca Denton, Haydn Beaton, David Donald, Christopher A. Luckhurst
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:7707-7710
The second part of this communication focuses on the resolution of issues surrounding the series of hydroxyamide phenoxypiperidine CCR3/H(1) dual antagonists described in Part I. This involved further structural exploration directed at reducing metab
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::4a2660289e12b8effe0ecbfde4d5f050
https://doi.org/10.1016/j.bmcl.2012.09.112
https://doi.org/10.1016/j.bmcl.2012.09.112
Autor:
David Cox, Alan V. Wallace, Anthony Ronald Cook, Anders Åberg, and Alan C. Tinker, John A. Tainer, David Cheshire, Haydn Beaton, Phil Mallinder, Ian Millichip, David J. Nicholls, Stephen A. St-Gallay, Sally L. Cooper, Robin J. Rosenfeld, Stephen Connolly, Andrew S. Arvai, Peter Hamley
Publikováno v:
Journal of Medicinal Chemistry. 47:3320-3323
4-Methylaminopyridine (4-MAP) (5) is a potent but nonselective nitric oxide synthase (NOS) inhibitor. While simple N-methylation in this series results in poor activity, more elaborate N-substitution such as with 4-piperidine carbamate or amide resul
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bbfd3e7f451affb3e932af18fb27fc41
https://doi.org/10.1021/jm031035n
https://doi.org/10.1021/jm031035n
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 11:1023-1026
3-Phenyl-3.4-dihydro-1-isoquinolinamine is a weak inhibitor of iNOS and nNOS. Structural variation of 5a results in inhibitors with a range of potency and selectivity for the NOS enzymes, including a potent and very selective iNOS inhibitor 5j.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::99a1b021ba648f38714dddd7c1e2b2aa
https://doi.org/10.1016/s0960-894x(01)00119-6
https://doi.org/10.1016/s0960-894x(01)00119-6
Publikováno v:
Tetrahedron Letters. 39:1227-1230
A variety of 1-amino-3,4-dihydroisoquinolines substituted at the 3-position and related thienopyridines were prepared by lithiation of ortho-methyl aromatic nitriles, addition to N-trimethylsilylimines and spontaneous cyclisation.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::db890902ba4080787da6ac3ba4dd38cd
https://doi.org/10.1016/s0040-4039(97)10736-5
https://doi.org/10.1016/s0040-4039(97)10736-5
Autor:
Mark, Furber, Lilian, Alcaraz, Christopher, Luckhurst, Ash, Bahl, Haydn, Beaton, Keith, Bowers, John, Collington, Rebecca, Denton, David, Donald, Elizabeth, Kinchin, Cathy, MacDonald, Aaron, Rigby, Rob, Riley, Matt, Soars, Brian, Springthorpe, Peter, Webborn
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(24)
The second part of this communication focuses on the resolution of issues surrounding the series of hydroxyamide phenoxypiperidine CCR3/H(1) dual antagonists described in Part I. This involved further structural exploration directed at reducing metab
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::b265960f1cf196e20fed3d284455964f
https://pubmed.ncbi.nlm.nih.gov/23116889
https://pubmed.ncbi.nlm.nih.gov/23116889
Autor:
Mark, Furber, Lilian, Alcaraz, Christopher, Luckhurst, Ash, Bahl, Haydn, Beaton, Keith, Bowers, John, Collington, Rebecca, Denton, David, Donald, Elizabeth, Kinchin, Cathy, MacDonald, Aaron, Rigby, Rob, Riley, Matt, Soars, Brian, Springthorpe, Peter, Webborn
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(24)
The discovery of potent small molecule dual antagonists of the human CCR3 and H(1) receptors is described for the treatment of allergic diseases, for example, asthma and allergic rhinitis. Optimizing in vitro potency and metabolic stability, starting
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::f02a7236d2b3e6e812e2998f262f09f1
https://pubmed.ncbi.nlm.nih.gov/23142617
https://pubmed.ncbi.nlm.nih.gov/23142617
Autor:
Stephen Connolly, Nigel Gensmantel, Peter Hamley, Richard P. Harrison, Paul Hartopp, Nigel Boughton-Smith, Timothy Nicholas Birkinshaw, Antonio Mete, Haydn Beaton, Sally L. Cooper, Austen Pimm, David Cheshire, Gunilla Andersson, Alan V. Wallace, Anders Åberg, Paul D. Leeson, John Dixon, David Cox, Timothy Jon Luker, Helena Käck, Ian Millichip, Steve St-Gallay, David J. Nicholls, Anne Cooper, Glen Andrews, Tony R. Cook
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(8)
By careful analysis of experimental X-ray ligand crystallographic protein data across several inhibitor series we have discovered a novel, potent and selective series of iNOS inhibitors exemplified by compound 8.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::899f9ebccc5f546ea9baf51a82b87d1e
https://pubmed.ncbi.nlm.nih.gov/21398123
https://pubmed.ncbi.nlm.nih.gov/21398123
Publikováno v:
ChemInform. 32
3-Phenyl-3,4-dihydro-1-isoquinolinamine is a weak inhibitor of iNOS and nNOS. Structural variation of 5a results in inhibitors with a range of potency and selectivity for the NOS enzymes, including a potent and very selective iNOS inhibitor 5j.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::416c875f93db2c455d8d3150c62aba2b
https://doi.org/10.1002/chin.200132147
https://doi.org/10.1002/chin.200132147
Autor:
Anant M. Ghelani, Alan V. Wallace, Nigel Boughton-Smith, Peter Hamley, Tinker Alan, Haydn Beaton, David J. Nicholls
Publikováno v:
ChemInform. 32
5-Substituted 7-amino-4,5-tetrahydrothieno[2,3-c]pyridines and 6-substituted 4-amino-6,7-dihydrothieno[3,2-c]pyridines were shown to be exceptionally potent inhibitors of inducible and neuronal nitric oxide synthase. Selectivity and potency could be
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::679edcf99439d10a1b14d445a5c7f14b
https://doi.org/10.1002/chin.200132150
https://doi.org/10.1002/chin.200132150