Zobrazeno 1 - 4
of 4
pro vyhledávání: '"Katharine Laura Collis"'
Autor:
Andrew Charlton, Stephen J. Medhurst, Laura J. Chambers, Livermore David, Brian Peter Slingsby, Andy Billinton, Lee William Page, Anton D. Michel, Daryl S. Walter, Jon Graham Anthony Steadman, Shilina Roman, Sadhana Patel, Elena Fonfria, Robert Gleave, Stefan Senger, Katharine Laura Collis, Andrew P. Moses, Sue D. Collins, Muna H. Abdi, Paul John Beswick, Clarisse L. Lejeune, David Kenneth Dean, Alexander J. Stevens
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:5080-5084
A computational lead-hopping exercise identified compound 4 as a structurally distinct P2X(7) receptor antagonist. Structure-activity relationships (SAR) of a series of pyroglutamic acid amide analogues of 4 were investigated and compound 31 was iden
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9a3ff37009bb76b9bfd50c27c623c06d
https://doi.org/10.1016/j.bmcl.2010.07.033
https://doi.org/10.1016/j.bmcl.2010.07.033
Autor:
Jon Graham Anthony Steadman, Daryl S. Walter, Beverley Smith, Lee Abberley, David Kenneth Dean, Elena Fonfria, Tiziana Scoccitti, Anton D. Michel, Sadhana Patel, Shilina Roman, Robert Gleave, Katharine Laura Collis, Stephen J. Medhurst, Andrew P. Moses, Aude Bebius, Paul John Beswick, Andy Billinton
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(22)
A backup molecule to compound 2 was sought by targeting the most likely metabolically vulnerable site in this molecule. Compound 18 was subsequently identified as a potent P2X(7) antagonist with very low in vivo clearance and high oral bioavailabilit
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5cdb4b6ee4ecb8615e490657bc2ef801
https://pubmed.ncbi.nlm.nih.gov/20934331
https://pubmed.ncbi.nlm.nih.gov/20934331
Autor:
Kim Winborn, Nicola Shuker, Benjamin R. Bellenie, Fiona McKay, Robert W. Ward, Andrew K. Takle, N. Paul King, Sharon Butler, Alessandra Gaiba, Jon Graham Anthony Steadman, Katharine Laura Collis, Jason Witherington, Rio Boatman, Tom D. Heightman, Lee Abberley, David Kenneth Dean, Alison I. Muir, Gareth J. Sanger
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(3)
As part of an on-going lead optimisation effort, a cross screening exercise identified an aryl sulphonyl amide hit that was optimised to afford a highly potent series of ghrelin receptor agonists.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0c4f34f29948982ea29b7786568744f8
https://pubmed.ncbi.nlm.nih.gov/19128969
https://pubmed.ncbi.nlm.nih.gov/19128969
Autor:
Graham Wadsworth, Jon Graham Anthony Steadman, Nicola Shuker, Lee Abberley, Michael A. Briggs, Helmut Kraus, N. Paul King, Tom D. Heightman, David Kenneth Dean, Katharine Laura Collis, Andrew K. Takle, Kim Winborn, Jason Witherington, Gareth J. Sanger, Fiona McKay, Sharon Butler, Alessandra Gaiba, Alison I. Muir
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(6)
A series of small molecule orally bioavailable ghrelin receptor agonists have been identified through systematic optimisation of a high throughput screening hit.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::28c166c3676ce1f0ac11de92a47952ea
https://pubmed.ncbi.nlm.nih.gov/18316188
https://pubmed.ncbi.nlm.nih.gov/18316188