Zobrazeno 1 - 9
of 9
pro vyhledávání: '"Jean E. Cottney"'
Autor:
Maurice Maidment, Angus John Morrison, Keneth Davies, Fiona Jeremiah, Grant Wishart, Alan Prosser, Robert A. Campbell, James Baker, Stuart Francis, Julia M. Adam, Ruth Fields, Susan Boyce, John K. Clark, Maureen Deehan, Jean E. Cottney, Takao Kiyoi, Iain Martin, Paul Ratcliffe, Kathryn Everett, Jurgen Schulz
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:2932-2937
Novel, low brain penetrant, orally bioavailable CB1 receptor agonists were designed starting from a mature lead series of potent brain penetrant CB1 receptor agonists. Increasing the calculated polar surface area was found to be a good strategy for r
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6d42884ec55ac32b481759aa8c65fa3f
https://doi.org/10.1016/j.bmcl.2012.02.048
https://doi.org/10.1016/j.bmcl.2012.02.048
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bac4fce3568bffcc8bec0c8ef27a0ea4
https://doi.org/10.1016/j.bmcl.2011.02.023
https://doi.org/10.1016/j.bmcl.2011.02.023
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ff623a5aaaefc52bb58196f1c7a44a87
https://doi.org/10.1016/j.bmcl.2010.10.093
https://doi.org/10.1016/j.bmcl.2010.10.093
Autor:
Grant Wishart, James Baker, Kazuya Yoshiizumi, Phillip M. Cowley, Mark York, Morag Ferguson, Glenn Walker, Takao Kiyoi, Jean E. Cottney, Jim Cairns, Petula McPhail, Fiona Jeremiah, Julia M. Adam, Jason Tierney, Andrea K. Houghton, Richard Morphy, Elizabeth Margaret Moir, Andrew Osprey
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:7327-7330
Bicyclic piperazine derivatives were synthesized as conformationally constrained analogs of N-alkyl piperazines and were found to be potent CB1 receptor agonists. The CB1 receptor agonist activity was dependent upon the absolute configuration of the
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fda2b173106078ac1cdfec6172f46ca0
https://doi.org/10.1016/j.bmcl.2010.10.061
https://doi.org/10.1016/j.bmcl.2010.10.061
Autor:
Julia Adams, Irina Beletskaya, Billy R. Martin, William L. Dewey, Jenny L. Wiley, Laura J. Sim-Selley, Anu Mahadevan, Jean E. Cottney, Raj K. Razdan, Forrest L. Smith, James Baker, Bijali Saha, David E. Hill, John Zerkowski
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 318:1230-1239
Presently, there are numerous structural classes of cannabinoid receptor agonists, all of which require solubilization for experimental purposes. One strategy for solubilizing water-insoluble tetrahydrocannabinols is conversion of the phenolic hydrox
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ccfad4d25c97de69976a222ad7fcfae0
https://doi.org/10.1124/jpet.106.104109
https://doi.org/10.1124/jpet.106.104109
Autor:
Silvia Broeders-Josten, Julia Oosterom, Jean E. Cottney, Antoon A. van der Doelen, Jeroen A.D.M. de Roos, Martin van Tilborg, Marcel Hermkens, Jos Cals, Jan P. G. Klomp, Vera de Kimpe, Angela King, Mario van der Stelt, James Baker, Susan Boyce, Ilse Pols-de Rooij
Publikováno v:
Journal of medicinal chemistry. 54(20)
Here, we report the identification and optimization of 1-(4-(pyridin-2-yl)benzyl)imidazolidine-2,4-dione derivatives as a novel chemotype with selective cannabinoid CB2 receptor agonist activity. 1 is a potent and selective cannabinoid CB2 receptor a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::54f473ef139387f958fde08febf68815
https://pubmed.ncbi.nlm.nih.gov/21923175
https://pubmed.ncbi.nlm.nih.gov/21923175
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f4a798f1ce53f1985c5d6f38960f220f
https://pubmed.ncbi.nlm.nih.gov/21316962
https://pubmed.ncbi.nlm.nih.gov/21316962
Autor:
James Baker, Julia M. Adam, Takao Kiyoi, Darren Edwards, Stuart Francis, Mark York, Andrea K. Houghton, Jean E. Cottney, Glenn Walker
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(16)
Novel tricyclic indole-3-carboxamides were synthesized as structurally restricted analogs of bicyclic indoles, and found to be potent CB1 cannabinoid receptor agonists. The CB1 agonist activity depended on the absolute configuration of the chiral cen
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1a2990a9ce0ca02e6ac880e959c5a035
https://pubmed.ncbi.nlm.nih.gov/20634067
https://pubmed.ncbi.nlm.nih.gov/20634067
Autor:
Morag Ferguson, Jean E. Cottney, Darren Edwards, James Baker, Jim Cairns, Paul Westwood, Fiona Jeremiah, Jason Tierney, Andrea K. Houghton, Mark York, Richard Goodwin, Phillip M. Cowley, Glenn Walker, Ashvin Mistry, Morag Easson, Iain Cumming, Richard Morphy, Wilson Caulfield, Julia M. Adam, Takao Kiyoi, Elizabeth Margaret Moir
Publikováno v:
MedChemComm. 1:54
A novel CB1 receptor agonist lead series was identified using a high-throughput screening approach. The initial screen afforded a single confirmed hit with poor water solubility. Structural variations were explored with the aim of introducing water s
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::50a9771d81118999bd825e636e929401
https://doi.org/10.1039/c0md00022a
https://doi.org/10.1039/c0md00022a