Zobrazeno 1 - 10
of 12
pro vyhledávání: '"Sarah Christine Hobbs"'
Autor:
W. Rycroft, George R. Marshall, Neil Collinson, Mark Stuart Chambers, Angus Murray Macleod, Gerard R. Dawson, John R. Atack, Susan M. Cook, Desmond O'Connor, Sarah Christine Hobbs, Pushpindar Ferris, Robert W. Carling
Publikováno v:
Journal of Medicinal Chemistry. 47:5829-5832
(3-tert-Butyl-7-(5-methylisoxazol-3-yl)-2-(1-methyl-1H-1,2,4-triazol-5-ylmethoxy)pyrazolo[1,5-d][1,2,4]triazine (13) has been identified as a functionally selective, inverse agonist at the benzodiazepine site of GABA(A) alpha5 receptors. 13 is orally
Publikováno v:
Journal of Liquid Chromatography & Related Technologies. 22:333-344
A series of 1,4-benzodiazepin-2-one CCKB receptor antagonists are reported in which substitution at C3 of the benzodiazepine by a phenyl-urea group bearing acidic moieties has generated a chiral centre. As one of these enantiomers is substantially mo
Autor:
Sarah Christine Hobbs, Smita Patel, Alison J. Smith, Stephen Robert Fletcher, Victor G. Matassa, Alan P. Watt, Raymond Baker, Stephen B. Freedman, Michael I. Graham, Mark Stuart Chambers
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 5:2303-2308
Acylsulphonamide analogues of the meta-tolylurea L-708,474 have been synthesised and evaluated as CCKB receptor antagonists. Such derivatives retain very high affinity and subtype selectivity for the CCKB receptor, and have good aqueous solubility. T
Autor:
Mark Stuart Chambers, Sarah Christine Hobbs, Richard G. Ball, Alan P. Watt, Stephen Robert Fletcher, Richard H. Herbert, Raymond Baker, Steven R. Thomas, Hugh M. Verrier
Publikováno v:
The Journal of Organic Chemistry. 59:1771-1778
The synthesis of (+)- and (-)-epibatidine (exo-2-(2-chloropyridin-5-yl)-7-azabicyclo[2.2.1]heptane) via reaction of 5-lithio-2-chloropyridine with (+)- and (-)-N-BOC-7-azabicyclo [2.2.1]heptan-2-one is described. The absolute configuration of the nat
Autor:
Alison J. Smith, Raymond Baker, P. J. Mitchell, Sarah Christine Hobbs, Stephen Robert Fletcher, Victor G. Matassa, Mark Stuart Chambers, Stephen B. Freedman, Alan P. Watt, Smita Patel
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 3:1919-1924
The C5-cyclohexyl analogue of the cholecystokinin type-B (CCKB) receptor antagonist L-365,260 has been prepared. This derivative has significantly higher CCKB affinity and markedly improved CCKB/CCKA receptor selectivity (6,500 v. 87-fold) than the p
Autor:
Raymond Baker, P. J. Mitchell, Stephen Robert Fletcher, Sarah Christine Hobbs, Mark Stuart Chambers
Publikováno v:
ChemInform. 24
The synthesis of the alkaloid epibatidine {exo-2-(2-chloro-5-pyridyl)-7-azabicyclo[2.2.1]heptane} in enantiomeric form involving, as the critical step, reaction or 5-lithio-2-chloropyridine with N-tert-butoxycarbonyl-7-azabicyclo[2.2.1]heptan-2-one i
Autor:
Sarah Christine Hobbs, Alan P. Watt, Mark Stuart Chambers, Raymond Baker, Hugh M. Verrier, Richard H. Herbert, Richard G. Ball, Stephen Robert Fletcher, Steven R. Thomas
Publikováno v:
ChemInform. 25
The synthesis of (+)- and (-)-epibatidine (exo-2-(2-chloropyridin-5-yl)-7-azabicyclo[2.2.1]heptane) via reaction of 5-lithio-2-chloropyridine with (+)- and (-)-N-BOC-7-azabicyclo [2.2.1]heptan-2-one is described. The absolute configuration of the nat
Autor:
Michael I. Graham, Alan P. Watt, Alison J. Smith, Victor G. Matassa, Raymond Baker, Stephen B. Freedman, Mark Stuart Chambers, Stephen Robert Fletcher, Smita Patel, Sarah Christine Hobbs
Publikováno v:
ChemInform. 27
Acylsulphonamide analogues of the meta-tolylurea L-708,474 have been synthesised and evaluated as CCKB receptor antagonists. Such derivatives retain very high affinity and subtype selectivity for the CCKB receptor, and have good aqueous solubility. T
Autor:
Helen Jane Szekeres, Matthew P. Braun, Angus Murray Macleod, Desmond O'Connor, Nicola Szeto, Robert James Maxey, Philip Jones, Keith A. Wafford, Mark Stuart Chambers, Brian P. Cato, Susan M. Cook, John R. Atack, Sarah Christine Hobbs
Publikováno v:
Bioorganicmedicinal chemistry letters. 16(4)
(3- tert -Butyl-7-(5-methylisoxazol-3-yl)-2-(1-methyl-1 H -1,2,4-triazol-5-ylmethoxy)pyrazolo[1,5- d ][1,2,4]triazine ( 1 ) was recently identified as a functionally selective, inverse agonist at the benzodiazepine site of GABA A α5 receptors and en
Autor:
Karen A. Maubach, Gerard R. Dawson, Susan M. Cook, Howard B. Broughton, Angus Murray Macleod, John R. Atack, Sarah Christine Hobbs, George R. Marshall, Mark Stuart Chambers, and Austin J. Reeve, Neil Collinson, Goplan V. Pillai
Publikováno v:
Journal of medicinal chemistry. 46(11)
In pursuit of a GABA(A) alpha5-subtype-selective inverse agonist to enhance cognition, a series of 6,7-dihydro-2-benzothiophen-4(5H)-ones has been identified as a novel class of GABA(A) receptor ligands. These thiophenes have higher binding affinity