Zobrazeno 1 - 9
of 9
pro vyhledávání: '"Wesley Peter Blackaby"'
Autor:
Wayne F. A. Sheppard, David S. Reynolds, Alison J. Smith, John R. Atack, Joanna Stanley, David James Hallett, Richard Thomas Lewis, Keith A. Wafford, Rowan A. Wilson, Timothy Blackburn, George R. Marshall, Wesley Peter Blackaby, Andrew Pike, Spencer J. Tye, Andrew Stephen Robert Jennings, Susan M. Cook, Pushpinder Ferris, Bindi Sohal
Publikováno v:
Journal of Medicinal Chemistry. 49:2600-2610
The development of a series of GABA(A) alpha2/alpha3 subtype selective pyridazine based benzodiazepine site agonists as anxiolytic agents with reduced sedative/ataxic potential is described, including the discovery of 16, a remarkably alpha3-selectiv
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3256a1392c1eb18c5f05fe4684c424b7
https://doi.org/10.1021/jm051144x
https://doi.org/10.1021/jm051144x
Autor:
Robert W. Carling, Wesley Peter Blackaby, Andrew Mitchinson, Sylvie Bourrain, Richard Thomas Lewis
Publikováno v:
Tetrahedron Letters. 47:2257-2260
Novel syntheses of 2,3,8-trisubstituted pyrido[2,3- d ]pyridazines and 2,3,5-trisubstituted pyrazino[2,3- d ]pyridazines are described. Two complementary routes to pyrido[2,3- d ]pyridazines were developed, the first of which began by constructing th
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::feaf8e32c8879e94ea5992207c5d8710
https://doi.org/10.1016/j.tetlet.2006.01.084
https://doi.org/10.1016/j.tetlet.2006.01.084
Autor:
Wesley Peter Blackaby, George R. Marshall, Richard Thomas Lewis, Simon Charles Goodacre, John R. Atack, David James Hallett, Leslie J. Street, Frances A. Bromidge, Andrew Pike, Alison J. Smith, David F. Tattersall, Keith A. Wafford, José L. Castro
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:1175-1179
Imidazo[1,2-a]pyrimidines are GABA(A) receptor benzodiazepine binding site ligands which can exhibit functional selectivity for the alpha(3) subtype over the alpha(1) subtype. SAR studies to optimize this functional selectivity are described.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0bac9dfff717bed7fe7f9f76e42c4294
https://doi.org/10.1016/j.bmcl.2005.11.112
https://doi.org/10.1016/j.bmcl.2005.11.112
Autor:
Wesley Peter Blackaby, Susan M. Cook, Alison J. Smith, Sarah Kelly, N. Brown, John R. Atack, Pushpinder Ferris, José L. Castro, Simon Charles Goodacre, Bindi Sohal, James Michael Crawforth, Joanna Stanley, Keith A. Wafford, David James Hallett, Andrew Pike, Richard Thomas Lewis, Leslie J. Street, George R. Marshall, Andrew Pate Owens
Publikováno v:
Journal of Medicinal Chemistry. 49:35-38
A series of high-affinity GABA(A) agonists with good oral bioavailability in rat and dog and functional selectivity for the GABA(A)alpha2 and -alpha3 subtypes is reported. The 7-trifluoromethylimidazopyrimidine 14g and the 7-propan-2-olimidazopyrimid
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f3b0dd96fcc598d89a504d83e49c338d
https://doi.org/10.1021/jm051065l
https://doi.org/10.1021/jm051065l
Autor:
H. Donald Burns, Martin R. Guscott, Andrew Stephen Robert Jennings, Sarah Almond, Simon Charles Goodacre, Gopalan V. Pillai, Alison J. Smith, Richard Thomas Lewis, Christine Ryan, Angus Murray Macleod, Andrew Pike, Leslie J. Street, Jacquelynn J. Cook, Steve Thomas, Terence G. Hamill, Suzanne Wood, Terry A. Brown, Wesley Peter Blackaby, Wai-Si Eng, Joanne Thomson
Amalgamation of the structure−activity relationship of two series of GlyT1 inhibitors developed at Merck led to the discovery of a clinical candidate, compound 16 (DCCCyB), which demonstrated excellent in vivo occupancy of GlyT1 transporters in rhe
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cfc2feaa39772a8555e55e31bcedea20
https://europepmc.org/articles/PMC4007840/
https://europepmc.org/articles/PMC4007840/
Autor:
Richard Thomas Lewis, Leslie J. Street, Alison J. Smith, Terry A. Brown, Joanne Thomson, Gopalan V. Pillai, Simon Charles Goodacre, Steve Thomas, Andrew Stephen Robert Jennings, Wesley Peter Blackaby, Andrew Pike
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(8)
Spleen tyrosine kinase (SYK) is a non-receptor cytosolic kinase. Due to its pivotal role in B cell receptor and Fc-receptor signaling, inhibition of SYK has been targeted in a variety of disease areas. Herein, we report the optimization of a series o
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::559a4a7179e6b967f6d202786a21d56c
https://pubmed.ncbi.nlm.nih.gov/19318248
https://pubmed.ncbi.nlm.nih.gov/19318248
Autor:
Andrew Mitchinson, Richard Thomas Lewis, Wesley Peter Blackaby, Sylvie Bourrain, Robert W. Carling
Publikováno v:
ChemInform. 37
Novel syntheses of 2,3,8-trisubstituted pyrido[2,3- d ]pyridazines and 2,3,5-trisubstituted pyrazino[2,3- d ]pyridazines are described. Two complementary routes to pyrido[2,3- d ]pyridazines were developed, the first of which began by constructing th
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::60236aa7f7e3504d21decb1a41ebe513
https://doi.org/10.1002/chin.200628142
https://doi.org/10.1002/chin.200628142
Autor:
Wesley Peter Blackaby, John R. Atack, David S. Reynolds, Jo Stanley, Simon Charles Goodacre, Susan M. Cook, Andrew Pike, Gerard R. Dawson, Rachael Lincoln, Richard Thomas Lewis, Keith A. Wafford, George R. Marshall, Ruth M. McKernan
Publikováno v:
Neuropharmacology. 50(6)
The cyclopyrrolone pagoclone binds with roughly equivalent high affinity (0.7e9.1 nM) to the benzodiazepine binding site of human recombinant GABAA receptors containing either an a1, a2, a 3o ra5 subunit. However, whereas it was a partial agonist at
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1ae203770241aa440ed7706382959ef0
https://pubmed.ncbi.nlm.nih.gov/16430927
https://pubmed.ncbi.nlm.nih.gov/16430927
Autor:
Wesley Peter Blackaby, Frances A. Bromidge, Ruth M. McKernan, Michael G. N. Russell, Keith A. Wafford, John R. Atack, Alison J. Smith, Richard Thomas Lewis, Leslie J. Street, José L. Castro
Publikováno v:
Bioorganicmedicinal chemistry letters. 15(22)
2,5-Dihydro-3H-pyrazolo[4,3-c]pyridin-3-ones are GABAA receptor benzodiazepine binding site ligands, which can exhibit functional selectivity for the α3 subtype over the α1 subtype. SAR studies to optimize this functional selectivity are described.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1fbe7534fdfd124abb03ee7112711769
https://pubmed.ncbi.nlm.nih.gov/16153832
https://pubmed.ncbi.nlm.nih.gov/16153832