Zobrazeno 1 - 9
of 9
pro vyhledávání: '"Tiziana Scoccitti"'
Autor:
Sahar Javed, Frank T. Coppo, Bronagh M. Heath, R. Dunsdon, David Norton, Emma S.L. Maskell, P. Theobald, Sanjeet Singh Sehmi, Tiziana Scoccitti, Robert W. Ward, Rio Hutchings, Deborah W. Chen, Leanne Cutler, Sally Redshaw, Laura Castelletti, David Matthew Wilson, Samuel Martin, David N. Hurst, Darrel J. Pemberton, John Skidmore, Richard A. Rutter, Emmanuelle Boucherat, Zeenat Atcha, Hannah E. Temple
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:3560-3563
A series of α7 nicotinic acetylcholine receptor full-agonists with a 1,3,4-oxadiazol-2-amine core has been discovered. Systematic exploration of the structure-activity relationships for both α7 potency and selectivity with respect to interaction wi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::51be7133cc767970bc7a50c751c021d3
https://doi.org/10.1016/j.bmcl.2012.03.040
https://doi.org/10.1016/j.bmcl.2012.03.040
Autor:
Adrian Hall, Tiziana Scoccitti, Christopher Budd, Alan Naylor, D. Anthony Rawlings, David N. Hurst, Alex W. Wilson, Nicholas Maughan Clayton, Thomas George Christopher Hayhow, Susan H. Brown, Wendy J. Winchester, Gerard Martin Paul Giblin, Paul Goldsmith
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:497-501
Herein we describe the medicinal chemistry programme to identify a potential back-up compound to the EP1 receptor antagonist GW848687X. This work started with the lipophilic 1,2-biaryl benzene derivative 4 which displayed molecular weight of 414.9 g/
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d247aa411a40ee1876a94dc9d1a8657f
https://doi.org/10.1016/j.bmcl.2008.11.032
https://doi.org/10.1016/j.bmcl.2008.11.032
Autor:
Adrian Hall, Susan H. Brown, Sadhana Patel, Andy Billinton, Gerard Martin Paul Giblin, Alan Naylor, Tiziana Scoccitti, David N. Hurst, Paul Goldsmith, Anita Chowdhury, Pamela J. Theobald
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:2684-2690
We describe the medicinal chemistry approach that generated a novel indole series of EP1 receptor antagonists. The SAR of this new template was evaluated and culminated in the identification of compound 12g which demonstrated in vivo efficacy in a pr
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f466feef99e2b2d9ba9ec68ab4f3aa5e
https://doi.org/10.1016/j.bmcl.2008.03.018
https://doi.org/10.1016/j.bmcl.2008.03.018
Autor:
D. Anthony Rawlings, Andy Billinton, Mairi Sime, Andrew John Eatherton, David N. Hurst, Anita Chowdhury, Charlotte Fieldhouse, Gerard Martin Paul Giblin, Adrian Hall, Tiziana Scoccitti, Pamela J. Theobald, Paul Goldsmith, Amanda C. Allan, Alan Naylor, Susan H. Brown
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(14)
We describe the discovery and optimization of a novel series of benzofuran EP(1) antagonists, leading to the identification of 26d, a novel nonacidic EP(1) antagonist which demonstrated efficacy in preclinical models of chronic inflammatory pain.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9f18e6d88765693cd451319b1486080d
https://pubmed.ncbi.nlm.nih.gov/21676612
https://pubmed.ncbi.nlm.nih.gov/21676612
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
Publikováno v:
Organic Letters. 2:3921-3923
A broad range of benzaldimines and ketimines can be hydrosilated efficiently, employing B(C(6)F(5))(3) as a catalyst in conjunction with PhMe(2)SiH. Spectral evidence supports the intermediacy of a silyliminium cation with a hydridoborate counterion
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::45fccfc882aa2834857e6ba2093fe8cf
https://doi.org/10.1021/ol006695q
https://doi.org/10.1021/ol006695q
Autor:
Paul Goldsmith, Mairi Gibson, Adrian Hall, Andy Billinton, Caroline F. Peet, David N. Hurst, Anita Chowdhury, Gerard Martin Paul Giblin, Wendy J. Winchester, Susan H. Brown, Tiziana Scoccitti, Nicholas Maughan Clayton, Alan Naylor, Alex W. Wilson
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(9)
We describe the medicinal chemistry programme that led to the identification of the EP1 receptor antagonist GSK269984A (8h). GSK269984A was designed to overcome development issues encountered with previous EP1 antagonists such as GW848687X and was fo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::32d9369ffffd0f115e687cec771f4d0d
https://pubmed.ncbi.nlm.nih.gov/19332369
https://pubmed.ncbi.nlm.nih.gov/19332369
Autor:
Adrian Hall, Gerard Martin Paul Giblin, David N. Hurst, Xiao Qing Lewell, Ian R. Kilford, Anita Chowdhury, Susan H. Brown, Alan Naylor, Rino A. Bit, Tiziana Scoccitti
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(5)
We describe the SAR, in terms of heterocyclic replacements, for a series of pyrazole EP 1 receptor antagonists. This study led to the identification of several aromatic heterocyclic replacements for the pyrazole in the original compound. Investigatio
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3cc22f992f03dae4b0833010ab0ad33c
https://pubmed.ncbi.nlm.nih.gov/18262416
https://pubmed.ncbi.nlm.nih.gov/18262416
Publikováno v:
ChemInform. 32
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::76a9689d3747d5f4ab9fac0f63e3512e
https://doi.org/10.1002/chin.200115090
https://doi.org/10.1002/chin.200115090