Zobrazeno 1 - 10
of 14
pro vyhledávání: '"Helen Feilden"'
Autor:
Anna Marie Easson, Yasuko Kiyoi, Steven Laats, Keneth Davies, Mark Reid, Stuart Francis, Helen Feilden, Grant Wishart, Peter C. Ray, Takao Kiyoi, Duncan McArthur
Publikováno v:
Tetrahedron Letters. 52:3421-3425
Tetrahydro-2H-[2]benzopyrano[3,4-c]pyrrol-3-ones and the related 3a-methyl-2,3,3a,4,5,9b-hexahydro-1H-benzo[e]isoindole analogues were synthesised by an intramolecular Diels–Alder reaction. The observed stereoselectivity was dependent upon the natu
Autor:
John Maclean, Lesley-Anne Nisbet, Helen Feilden, Olaf Nimz, Duncan McArthur, Ronnie Palin, Lynn Abernethy, Hazel McLuskey, Thomas R. Clarkson, Darren Edwards, Deborah McGregor, Anna-Marie Easson, Katy Everett, Paul Ratcliffe, Heather Tracey, Maureen Dempster, Littlewood Peter Thomas Albert, Glenn Walker
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:2559-2563
Optimization of a water soluble, moderately potent lead series of isoxazole-3-carboxamides was conducted, affording a compound with the requisite balance of potency, solubility and physicochemical properties for in vivo use. Compound 8e was demonstra
Autor:
Ronald Palin, Hardy Sundaram, Philip S. Jones, David Vrolijk, Louise Evans, Mark A. Weston, David R. Barn, Grove Simon James Anthony, Helen Feilden, John K. Clark, J. Cottney, Marc Crockatt, Alasdair R.C. Smith, Grant Wishart, Paul Wren, Phillip M. Cowley, Richard Morphy, Frank Griekspoor, Richard R. Goodwin, Andrea K. Houghton
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:589-593
A series of 3-phenoxypropyl piperidine analogues have been discovered as novel ORL1 receptor agonists. Structure-activity relationships have been explored around the 3-phenoxypropyl region with several potent and selective analogues identified.
Autor:
Helen Feilden, Anne Cleasby, Neil Taylor, Alan J. Wonacott, Paul W. Smith, Derek N. Evans, Steven L. Sollis, Peter D. Howes
Publikováno v:
European Journal of Medicinal Chemistry. 34:225-234
Two methods for the synthesis of 4-acetylamino benzoic acids substituted at the 3-position with imidazoles are described. Many of the compounds are inhibitors of influenza virus sialidases with levels of activity similar to the recently described 4-a
Autor:
Jean E. Cottney, Paul Ratcliffe, James Baker, Ruth Fields, John K. Clark, Helen Feilden, Darren Edwards, Grant Wishart, Fiona Jeremiah, Maureen Deehan, Angus John Morrison, Stuart Francis, Louise Evans, Alan Prosser, Robert A. Campbell, Ola Epemolu, Jurgen Schulz, Keneth Davies, Takao Kiyoi, Duncan McArthur, Julia M. Adam, Anna-Marie Easson
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(6)
Novel 3-(1H-indol-3-yl)-1,2,4-oxadiazoles and -thiadiazoles were synthesized and found to be potent CB1 cannabinoid receptor agonists. The oral bioavailability of these compounds could be dramatically improved by optimization studies of the side chai
Autor:
Lynn Abernethy, Quynhchi Pham, Helen Feilden, Olaf Nimz, Yajing Rong, Michael Ohlmeyer, Anna-Marie Easson, David A. Dunn, Heather Tracey, Littlewood Peter Thomas Albert, Steve Kultgen, Lesley-Anne Nisbet, John Maclean, Maureen Dempster, Duncan McArthur, Robert Swanson, Melanie Sammons, Ronnie Palin, Andrew Laird Roughton, Darren Edwards, Kenneth S. Cameron, Deborah McGregor, Paul Ratcliffe, Irina Neagu, Hazel McLuskey, Koc-Kan Ho, Katy Everett, Thomas R. Clarkson, Glenn Walker, Nasrin Ansari
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(15)
Systematic optimisation of a poorly soluble lead series of isoxazole-3-carboxamides was conducted. Substitution of the 4-position with specific polar functionality afforded the requisite balance of potency, solubility and physicochemical properties.
Autor:
Michael Ohlmeyer, Yajing Rong, Katy Everett, Robert Swanson, Nasrin Ansari, Duncan McArthur, Kenneth S. Cameron, Quynhchi Pham, Irina Neagu, Heather Tracey, Darren Edwards, John Maclean, Maureen Dempster, Thomas R. Clarkson, Hazel McLuskey, Koc-Kan Ho, Helen Feilden, Paul Ratcliffe, David A. Dunn, Andrew Laird Roughton, S.A. Neale, Steve Kultgen, Glenn Walker, Littlewood Peter Thomas Albert, Melanie Sammons, Ronald Palin, Lynn Abernethy, Anna-Marie Easson, Deborah McGregor, Lesley-Anne Nisbet
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(3)
Optimisation of a screening hit incorporating both TRPV1 activity and solubility was conducted. Substitution of the isoxazole-3-carboxamide with the bespoke 1S, 3R-3-aminocyclohexanol motif afforded the requisite balance of potency and solubility. Co
Autor:
Helen Feilden, Paul W. Smith, Peter D. Howes, Derek N. Evans, Neil Taylor, Anne Cleasby, Alan J. Wonacott, Steven L. Sollis
Publikováno v:
ChemInform. 30
Two methods for the synthesis of 4-acetylamino benzoic acids substituted at the 3-position with imidazoles are described. Many of the compounds are inhibitors of influenza virus sialidases with levels of activity similar to the recently described 4-a
Autor:
Duncan McArthur, Alasdair R.C. Smith, Niall M. Hamilton, Louise Evans, Ronald Palin, Helen Feilden, Dan Fletcher, Grant Wishart, Aaron Sutherland, Philip S. Jones, Mark A. Weston, Paul Ratcliffe, John K. Clark, Brian Montgomery, Andrea K. Houghton
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(22)
A knowledge based approach has been adopted to identify novel NOP receptor agonists with simplified hydrophobes. Substitution of the benzimidazol-2-one piperidine motif with a range of hydrophobic groups and pharmacophore guided bio-isosteric replace
Autor:
Grant Wishart, Brian Montgomery, Anton Bom, Ronald Palin, Mark A. Weston, Andrea K. Houghton, Philip S. Jones, Helen Feilden, John K. Clark, Louise Evans
Publikováno v:
Bioorganicmedicinal chemistry. 15(4)
A series of 3-phenoxypropyl piperidine benzimidazol-2-one analogues have been discovered as novel NOP receptor agonists. Structure-activity relationships have been explored via N-3 substitution of the benzimidazol-2-one with a range of functionality.