Zobrazeno 1 - 7
of 7
pro vyhledávání: '"Thomas R. Clarkson"'
Autor:
Yasuko Kiyoi, Phillip M. Cowley, Ian Carlyle, James R. Baker, Thomas R. Clarkson, Grant Wishart, Dawn Osbourn, Iain J. Martin, Kirsteen Buchanan, Darren Edwards, Nick Ward, Maureen Deehan, John K. Clark, Glenn Walker
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:2034-2039
The pharmacokinetic based optimisation of a novel series of indole-2-carboxamide antagonists of the cannabinoid CB(1) receptor is disclosed. Compound 24 was found to be a highly potent and selective cannabinoid CB(1) antagonist with high predicted hu
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5d24af231886a7db08d0f88ddcb8863c
https://doi.org/10.1016/j.bmcl.2011.02.019
https://doi.org/10.1016/j.bmcl.2011.02.019
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8687a4faf5d28c80274d767145e3b914
https://doi.org/10.1016/j.bmcl.2011.01.112
https://doi.org/10.1016/j.bmcl.2011.01.112
Autor:
Daphne Szeto, Doris F. Cully, Scott B. Hoyt, Ning Ren, Elaine Tung, Charlene Bopp, Jack Gibson, Gino Salituro, Clare London, Jiaqiang Cai, Amjad Ali, Qing Chen, Andrea Sok, Simone Belshaw, Carrie Ann Maxwell, Mark Rosenbach, Gaochao Zhou, Gail Forrest, Tian-Quan Cai, Daniel R. McMasters, Lee-Yuh Pai, Nelo R. Rivera, Sloan Stribling, Emma Carswell, Richard Hajdu, Robinson John E, Andrew J. Cooke, Jeff Kuethe, Tom Wisniewski, Joe Metzger, Thomas R. Clarkson, Gui-Bai Liang, Mary Struthers, Jim Tata, Mike E. Lassman, Lindsay Brown, Wei Tang, Theresa McLaughlin, Xiuying Ma, Nicole Buist, Kun Liu, Joe Clemas, D. Jonathan Bennett, Andreas Verras, Min K. Park, Yusheng Xiong, John Maclean, Jose Castro-Perez
We report the discovery of a benzimidazole series of CYP11B2 inhibitors. Hit-to-lead and lead optimization studies identified compounds such as 32, which displays potent CYP11B2 inhibition, high selectivity versus related CYP targets, and good pharma
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::02bdb44414988404f1b182298b88bcd9
https://europepmc.org/articles/PMC4434468/
https://europepmc.org/articles/PMC4434468/
Publikováno v:
Tetrahedron Letters. 43:1583-1585
11-(1,2,5,6-Tetrahydro-1-methyl-3-pyridinyl)-5-methyl-5 H -dibenzo[ b , e ][1,4]diazepine on heating in conc. HBr afforded trans -5-(2-aminophenyl)-1,3,4,4a,5,10a-hexahydro-2-methylbenzo[ b ][1,6]naphthyridin-10(2 H )-one in one step. The isomer 11-(
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::51f81a31635562396b10e59999926db2
https://doi.org/10.1016/s0040-4039(02)00063-1
https://doi.org/10.1016/s0040-4039(02)00063-1
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.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d5d0b565a24df327effc59eb4784735f
https://pubmed.ncbi.nlm.nih.gov/21723725
https://pubmed.ncbi.nlm.nih.gov/21723725
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f76a2109a2b4a6f8968b66029d3564f8
https://pubmed.ncbi.nlm.nih.gov/21236666
https://pubmed.ncbi.nlm.nih.gov/21236666
Autor:
Ian Carlyle, Elise C. O’Donnell, Daniel Spinks, Gayle Spinks, Anne M. Thomson, Thomas R. Clarkson, Wilson Caulfield, Fiona Thomson, James J. Strain, David Robert Jaap, Mark Reid, Fiona Cusick, Zoran Rankovic, Richard Goodwin, Grant Wishart, Ola Epemolu, Robert Gilfillan, Jeremy Presland
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(12)
Antagonists of the 5-HT(6) receptor have been shown to improve cognitive function in a wide range of animal models and as such may prove to be attractive agents for the symptomatic treatment of cognitive disorders such as Alzheimer's disease (AD) and
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::73b0955b33c6696bb0cdcfcaee845bac
https://pubmed.ncbi.nlm.nih.gov/20471831
https://pubmed.ncbi.nlm.nih.gov/20471831