Zobrazeno 1 - 3
of 3
pro vyhledávání: '"Helene Sahri"'
Autor:
Nicola Arnold, Julie Christie, Sandra Haberthuer, Roger J. Taylor, Alastair Denholm, Mark Keenan, Julia Hatto, Mark Mercer, Lyndon Nigel Brown, Clive Mccarthy, Neil John Press, Helen Oakman, Andrew R. Tuffnell, Morris Tweed, Alexandre Trifilieff, Robert Cheung, Joseph D. Fullerton, Thomas H. Keller, David Beer, Helene Sahri, Pamela Tranter
Publikováno v:
Journal of Medicinal Chemistry. 58:6747-6752
Herein we describe the optimization of a series of PDE4 inhibitors, with special focus on solubility and pharamcokinetics, to clinical compound 2, 4-(8-(3-fluorophenyl)-1,7-naphthyridin-6-yl)transcyclohexanecarboxylic acid. Although compound 2 produc
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3f1713cba513710940b786b9defedf19
https://doi.org/10.1021/acs.jmedchem.5b00902
https://doi.org/10.1021/acs.jmedchem.5b00902
Autor:
Helene Sahri, Julie Christie, Neil John Press, Mark Keenan, Sandra Haberthuer, Morris Tweed, Andrew R. Tuffnell, Mark Mercer, Joseph D. Fullerton, John R. Fozard, Thomas H. Keller, Nicola Elaine Press, Lyndon Nigel Brown, Roger J. Taylor, Clive Mccarthy, Julia Hatto, Robert Cheung, Pamela Tranter
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:3081-3085
The synthesis and SAR of 5-heterocycle-substituted aminothiazole adenosine receptor antagonists is described. Several compounds show high affinity and selectivity for the A2B and A3 receptors. One compound (5f) shows good ADME properties in the rat a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3947523839cef2983228f572e9013e7c
https://doi.org/10.1016/j.bmcl.2005.04.021
https://doi.org/10.1016/j.bmcl.2005.04.021
Autor:
Sandra Haberthuer, Trixie Wagner, Lyndon Nigel Brown, Julia Hatto, Nicola Arnold, Clive Mccarthy, Julie Christie, John R. Fozard, Helene Sahri, Helen Oakman, Thomas H. Keller, Roger J. Taylor, Robert Cheung, Mark Keenan, Neil John Press, Joseph D. Fullerton, Andrew R. Tuffnell, Alexandre Trifilieff, John W. Tyler, David Beer, Alastair Denholm, Morris Tweed, Mark Mercer, Pamela Tranter
Publikováno v:
Journal of medicinal chemistry. 55(17)
The solubility-driven optimization of a series of 1,7-napthyridine phosphodiesterase-4 inhibitors is described. Directed structural changes resulted in increased aqueous solubility, enabling superior pharmacokinetic properties with retention of PDE4
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::817ed3d0e78a77ec4c0cc42ee5087e6b
https://pubmed.ncbi.nlm.nih.gov/22889281
https://pubmed.ncbi.nlm.nih.gov/22889281