Zobrazeno 1 - 8
of 8
pro vyhledávání: '"Anna-Marie Easson"'
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:
Takao Kiyoi, Mark Reid, Stuart Francis, Keneth Davies, Steven Laats, Duncan McArthur, Anna-Marie Easson, Yasuko Kiyoi, Gary Tarver, Wilson Caulfield, Kirsty Gibson, Grant Wishart, Angus J. Morrison, Julia M. Adam, Peter Ray
Publikováno v:
Tetrahedron Letters. 52:3413-3416
Autor:
Robert A. Campbell, Angus John Morrison, Julia M. Adam, Daniel Ecker, Stuart Francis, James Baker, Anna-Marie Easson, Fiona Jeremiah, Ola Epemolu, Takao Kiyoi, Roberta Bursi, Duncan McArthur, Jurgen Schulz, Darren Edwards, Paul Passier, Maureen Deehan, Paul Westwood, Joanna Udo de Haes, Peter G. Schnabel, Jean E. Cottney, John K. Clark, Glenn Walker, Paul Harradine, Heinz Steinbrede, Paul Ratcliffe, Grant Wishart, Ruth Fields, Jack Pick, Louise Evans
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:2541-2546
We report an expansion of the structure-activity relationship (SAR) of a novel series of indole-3-heterocyclic CB1 receptor agonists. Starting from the potent but poorly soluble lead, 1, a rational approach was taken in order to balance solubility, h
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:
Julia M. Adam, Kazuya Yoshiizumi, Paul Ratcliffe, Neil S. Keddie, Takao Kiyoi, Grant Wishart, Jurgen Schulz, Duncan McArthur, Angus John Morrison, John K. Clark, Karsten Meyer, James Baker, Jean E. Cottney, Maureen Deehan, Robert A. Campbell, Ruth Fields, Anna-Marie Easson, Stuart Francis, Fiona Jeremiah
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:506-509
Novel indole-3-heterocycles were designed and synthesized and found to be potent CB1 receptor agonists. Starting from a microsomally unstable lead 1, a bioisostere approach replacing a piperazine amide was undertaken. This was found to be a good stra
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