Zobrazeno 1 - 10
of 14
pro vyhledávání: '"Maureen Dempster"'
Autor:
Anja Jestel, Stephan Krapp, Maureen Dempster, Xavier Fradera, Susanna Nagel, Emma Carswell, Andrew J. Cooke, William Hamilton, Bert Kazemier, Arthur Oubrie
Publikováno v:
Acta Crystallographica Section F Structural Biology and Crystallization Communications. 68:404-408
Factor XI (FXI) is a key enzyme in the coagulation pathway and an attractive target for the development of anticoagulant drugs. A small number of high-resolution crystal structures of FXIa in complex with small synthetic inhibitors have been publishe
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:
John Bruin, William Hamilton, Emma Kinghorn, Kenneth S. Cameron, Paul Westwood, Jiaqiang Cai, Kathryn Everett, Clive Long, Maureen Dempster, Chris Claxton, Xavier Fradera, D. Jonathan Bennett, Robinson John E, Simone Belshaw, Philip Jones, Wullie Arbuckle, Mark Baugh, Iain Martin
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:932-935
Based on the theoretical understanding of the in vivo lysosomotropism, by adjusting the pka of basic nitrogen containing cathepsin S inhibitors, a set of compounds with pka 6–8 were identified to have excellent cell based Lip10 activity, yet avoidi
Autor:
Hortense Deronzier, Cecile Dorleans, John Waller, Laurent Saniere, Andre Fouquet, Fiona Elizabeth Andrews, Mark Baugh, J.C.M. Uitdehaag, George McGarry, Phil Jones, Ann Mitchell, Emma Kinghorn, Eric Nicolai, Wilson Caulfield, Zoran Rankovic, Dominique Potin, Mario van Zeeland, Wullie Arbuckle, Jennifer Kerr, Jiaqiang Cai, Mark Wheaton Anderson, Iain Martin, Maureen Dempster, Ashvin Mistry, François Chevallier, William Finlay, Clive Long, Robinson John E, Xavier Fradera, Paul Westwood, Iain Cumming
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:6237-6241
Several structure-guided optimisation strategies were explored in order to improve the hERG selectivity profile of cathepsin K inhibitor 1 , whilst maintaining its otherwise excellent in vitro and in vivo profile. Ultimately, attenuation of c log P a
Autor:
D. Jonathan Bennett, Kenneth S. Cameron, John Bruin, Mario van Zeeland, Xavier Fradera, J.C.M. Uitdehaag, Emma Kinghorn, Jiaqiang Cai, Maureen Dempster, Paul Westwood, Lucy Popplestone, Mark Baugh, Robinson John E, William Hamilton, Clive Long
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:4507-4510
Using computer aided modelling studies, a new extended P2/S2 interaction was identified. This extended region can accommodate a variety of functional groups, such as aryls and basic amines. It was discovered that the N3 nitrogen of the pyrimidine-2-c
Autor:
T.M. Meulemans, Jonathan Gillespie, D. Jonathan Bennett, Darcey Black, Ann Mitchell, Kenneth S. Cameron, J.C.M. Uitdehaag, Maurice Maidment, Mario van Zeeland, Fiona Elizabeth Andrews, Sylviane Boucharens, Allard Kaptein, Maureen Dempster, Emma Kinghorn, Mark Baugh, Jiaqiang Cai, Philip Jones, Zoran Rankovic, Paul Westwood, Martijn Bastiani, Iain Martin, Iain Cumming, Leon van Berkom, Paul Vink, Paul Scullion, Xavier Fradera, John Bruin, Robinson John E, William Hamilton, Clive Long
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:4350-4354
6-Phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile analogues were identified as potent and selective cathepsin S inhibitor against both purified enzyme and in human JY cell based cellular assays. This core has a very stable thio-trapping nitrile war-h
Autor:
Eric Nicolai, Clive Long, Ann Mitchell, Maureen Dempster, William Hamilton, Jennifer Kerr, Cecile Dorleans, Iain Martin, Paul Scullion, Hortense Deronzier, John Bruin, Emma Hamilton, Zoran Rankovic, Andre Fouquet, John Robinson, John Waller, Laurent Saniere, Mark Baugh, Fiona Andrews, Jiaqiang Cai, Joost C.M. Uitdehaag, Wilson Caulfield, Dominique Potin, Ashvin Mistry, François Chevallier, Paul Westwood, Emma Kinghorn, George McGarry, Iain Cumming, Mario van Zeeland, X. Fradera
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:1524-1527
Morphing structural features of HTS-derived chemotypes led to the discovery of novel 2-cyano-pyrimidine inhibitors of cathepsin K with good pharmacokinetic profiles, for example, compound 20 showed high catK potency (IC(50)=4nM), >580-fold selectivit
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:
Leontien den Hoed, A. Mieke H. Boots, Ethan Grant, Heather J. McKinnon, Kieran McGregor, Monika Gorecka, Jonathan Bennett, Mark Baugh, John Bruin, William Hamilton, Christopher Robert James Claxton, Paul Vink, M. David Percival, Kalpit A. Vora, Clive Long, Marie-Jose van Lierop, Maureen Dempster, Emma Kinghorn, Darcey Black, Jiaqiang Cai, Paul Westwood
Publikováno v:
Journal of autoimmunity. 36(3-4)
The purpose of the study was to examine the potential of inhibition of cathepsin S as a treatment for autoimmune diseases. A highly selective cathepsin S inhibitor, CSI-75, was shown to upregulate levels of the cathepsin S substrate, invariant chain