Zobrazeno 1 - 10
of 40
pro vyhledávání: '"Barry Sidney Orlek"'
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.
Publikováno v:
Tetrahedron. 65:5503-5512
Stable silylketenes, prepared by rhodium-catalysed decomposition of silyldiazoketones, undergo addition/cyclocondensation sequences with aminophenols and aminomalonate to give α-silylalkylbenzoxazoles and oxazoles, respectively. The silicon can be r
Autor:
Peter Henry Milner, Barry Sidney Orlek, James Matthew Bailey, Anthony Huxley, Gordon Bruton, Vicky Johnstone, Geoffrey Stemp
Publikováno v:
Synlett. 2009:1051-1054
An efficient four-step synthesis (requiring no purification) of Boc-protected 4,4'-dipiperidinyl ethers is described.
Autor:
David Matthew Wilson, Alison M. Ray, Andrew D. Medhurst, Robert P. Davis, Ciaran M. Regan, Andrew G. Foley, Teresa Heslop, Sandrine Ociepka, Michael A. Briggs, Trevor White, Barry Crook, Barry Sidney Orlek, Stephen J. Medhurst, Andrew R. Calver, Brenda K. Trail, Iain P. Chessell, Becky Sargent, Tania O. Stean, Joanne Schogger, Neil Upton, Warren D. Hirst, Gordon Bruton, John B. Davis
Publikováno v:
Biochemical Pharmacology. 73:1182-1194
GSK207040 (5-[(3-cyclobutyl-2,3,4,5-tetrahydro-1 H -3-benzazepin-7-yl)oxy]- N -methyl-2-pyrazinecarboxamide) and GSK334429 (1-(1-methylethyl)-4-({1-[6-(trifluoromethyl)-3-pyridinyl]-4-piperidinyl}carbonyl)hexahydro-1 H -1,4-diazepine) are novel and s
Autor:
John David Harling, Barry Sidney Orlek
Publikováno v:
Tetrahedron. 54:14905-14912
3-Substituted hexahydroindeno[2,1-b]pyrroles were prepared in a stereoselective manner in high yield via an intramolecular azomethine ylide cycloaddition. Olefin geometry in the ylide precursor controlled the stereochemistry at the 3-position.
Autor:
Frederick Cassidy, Julie Hawkins, Barry Sidney Orlek, Steven Mark Bromidge, Christopher B. Naylor, Frank Brown, Michael S. G. Clark, Loudon Julia Mary, Michael S. Hadley, Graham J. Riley, Steven Dabbs
Publikováno v:
Journal of Medicinal Chemistry. 40:4265-4280
Loss of cholinergic function is believed to be implicated in the cognitive decline associated with senile dementia of the Alzheimer type (SDAT). The disease is characterized by progressive loss of muscarinic receptors located on nerve terminals while
Autor:
Barry Sidney Orlek, Eleanor A. Crowe
Publikováno v:
Journal of the Chemical Society, Perkin Transactions 1. :2775-2778
The trans-1-anilino-2-aminoindane derivative 2a derived from the adduct 1 of indene and N,N-dichlorourethane is suitably functionalised for further elaboration to give novel fused ring systems. This report describes the use of 2a to provide access to
Autor:
Julie Hawkins, Barry Sidney Orlek, Graham J. Riley, Emma J. Collings, Richard E. Faulkner, Frederick Cassidy, Michael S. G. Clark
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 4:1411-1414
Replacement of the ester group in methyl quinuclidine-3-car☐ylate1 with a 1,2,4-triazine ring afforded the high affinity muscarinic partial agonist6a. Analogues7a,7b and7d which incorporate the 1-azabicyclo[2.2.1]heptane ring also display high affi
Autor:
Frederick Cassidy, Richard E. Faulkner, Steven Mark Bromidge, Barry Sidney Orlek, Graham J. Riley, Michael S. G. Clark, Michael S. Hadley, Geoffrey Stemp
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 4:1185-1190
Constraining the 1,2,5,6-tetrahydropyridine ring of arecoline 1a and the related muscarinic agonists 1b–e by replacing the N-methyl group by an ethano bridge between the nitrogen and the C5-position afforded compounds 2a–e . These compounds have
Autor:
Barry Sidney Orlek, Graham J. Riley, Richard E. Faulkner, Steven Mark Bromidge, Frank Brown, Michael S. G. Clark, Frederick Cassidy, Loudon Julia Mary, Steven Dabbs, Emma J. Collings
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 4:557-562
The combination of N-methoxy imidoyl halide and nitrile moieties with the 1,2,5,6-tetrahydropyridine ring system afforded a novel series of potent muscarinic agonists. Members of this class, exemplified by the imidoyl nitriles 2c and 3c , show favour