Zobrazeno 1 - 10
of 78
pro vyhledávání: '"Alan D. Borthwick"'
Autor:
David J. Nutt, Robin J. Tyacke, Meg Spriggs, Vanessa Jacoby, Alan D. Borthwick, Delia Belelli
Publikováno v:
Nutrients. 14(18)
The consumption of alcohol is associated with well-known health harms and many governments worldwide are actively engaged in devising approaches to reduce them. To this end, a common proposed strategy aims at reducing alcohol consumption. This approa
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5e91761abd9b58550e55a6d9dee8a14e
https://pubmed.ncbi.nlm.nih.gov/36145137
https://pubmed.ncbi.nlm.nih.gov/36145137
Autor:
Alan D. Borthwick
Publikováno v:
Mini-Reviews in Medicinal Chemistry. 17:572-582
BACKGROUND The design, medicinal chemistry, pharmacokinetics and development of the highly selective α2-adrenoceptor antagonist fluparoxan are reviewed. METHOD The drug's activity and selectivity in vitro, its efficacy in animals and its excellent o
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::76ecd4babc8a670c72cea5683ead8933
https://doi.org/10.2174/1389557516666160321115041
https://doi.org/10.2174/1389557516666160321115041
Publikováno v:
Bioorganic & Medicinal Chemistry
Graphical abstract
Retinoic acid receptors (RARs) α, β, and γ are members of the nuclear receptor superfamily. Compounds which bind to and activate the RARs are termed retinoids which regulate a wide variety of biological processes such as ve
Retinoic acid receptors (RARs) α, β, and γ are members of the nuclear receptor superfamily. Compounds which bind to and activate the RARs are termed retinoids which regulate a wide variety of biological processes such as ve
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2bd24e85916fd8df1e0b05c476953b63
https://doi.org/10.1016/j.bmc.2020.115664
https://doi.org/10.1016/j.bmc.2020.115664
Autor:
Carl Hobbs, S. Barret Kalindjian, John Grist, Thomas Carlstedt, Jonathan Corcoran, Maria B. Goncalves, Peter Mumford, Christopher I. Jarvis, Earl Clarke, Mark Trevor Mills, Jane Theresa Brown, Alan D. Borthwick, Julian Jack, Thomas Pitcher
Publikováno v:
Bioorganic & Medicinal Chemistry Letters
Oxadiazole replacement of an amide linkage in an RARα agonist template 1, followed by lead optimisation, has produced a highly potent and selective RARβ agonist 4-(5-(4,7-dimethylbenzofuran-2-yl)-1,2,4-oxadiazol-3-yl)benzoic acid (10) with good ora
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5cac033e762913965dd8ab36d045c10c
https://doi.org/10.1016/j.bmcl.2019.05.058
https://doi.org/10.1016/j.bmcl.2019.05.058
Autor:
Earl, Clarke, Christopher I, Jarvis, Maria B, Goncalves, S Barret, Kalindjian, David R, Adams, Jane T, Brown, Jason J, Shiers, David M A, Taddei, Elodie, Ravier, Stephanie, Barlow, Iain, Miller, Vanessa, Smith, Alan D, Borthwick, Jonathan P T, Corcoran
Publikováno v:
Bioorganic & Medicinal Chemistry
Graphical abstract
A ligand-based virtual screening exercise examining likely bioactive conformations of AM 580 (2) and AGN 193836 (3) was used to identify the novel, less lipophilic RARα agonist 4-(3,5-dichloro-4-ethoxybenzamido)benzoic acid 5
A ligand-based virtual screening exercise examining likely bioactive conformations of AM 580 (2) and AGN 193836 (3) was used to identify the novel, less lipophilic RARα agonist 4-(3,5-dichloro-4-ethoxybenzamido)benzoic acid 5
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::a651db96aeac6253440f0f177d2dd404
https://pubmed.ncbi.nlm.nih.gov/29288071
https://pubmed.ncbi.nlm.nih.gov/29288071
Autor:
Savvas Kleanthous, Alan D. Borthwick, David Brown, Cynthia L. Burns-Kurtis, Matthew Campbell, Laiq Chaudry, Chuen Chan, Marie-Olive Clarte, Máire A. Convery, John D. Harling, Eric Hortense, Wendy R. Irving, Stephanie Irvine, Anthony J. Pateman, Angela N. Patikis, Ivan L. Pinto, Derek R. Pollard, Theresa J. Roethka, Stefan Senger, Gita P. Shah, Gary J. Stelman, John R. Toomey, Nigel S. Watson, Robert I. West, Caroline Whittaker, Ping Zhou, Robert J. Young
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:618-622
Structure and property based drug design was exploited in the synthesis of sulfonamidopyrrolidin-2-one-based factor Xa inhibitors, incorporating neutral and basic monoaryl P4 groups, ultimately producing potent inhibitors with effective levels of ant
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d3c703cdb093d395dc4c312cc73a2b70
https://doi.org/10.1016/j.bmcl.2009.11.077
https://doi.org/10.1016/j.bmcl.2009.11.077
Autor:
John Liddle, Alan D. Borthwick
Publikováno v:
Medicinal Research Reviews. 31:576-604
A short, efficient and highly stereoselective synthesis has been developed for a series of 6-indanyl-3-alkyl-7-aryl/heterocyclic-(3R, 6R, 7R)-2, 5-diketopiperazine amides that are potent and selective oxytocin (OT) antagonists. Property-based design
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5929ead34a4e70d9c4b3bbd80e33643f
https://doi.org/10.1002/med.20193
https://doi.org/10.1002/med.20193
Autor:
Alan D. Borthwick, Marie Charbaut, Robert J. Young, Máire A. Convery, Ivan Leo Pinto, Andrew M. Mason, Weston Helen Elisabeth, Matthew Campbell, David W. Brown, Anthony J. Pateman, Henry Anderson Kelly, Derek Pollard, Shah Gita Punjabhai, John R. Toomey, N. Paul King, Stefan Senger, Eric Hortense, Ping Zhou, Hawa Diallo, Nigel S. Watson, Wendy R. Irving, Angela Patikis, Cynthia L. Burns-Kurtis, Savvas Kleanthous, Chuen Chan
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:28-33
Structure and property based drug design was exploited in the synthesis of sulfonamidopyrrolidin-2-one-based factor Xa (fXa) inhibitors, incorporating basic biaryl P4 groups, producing highly potent inhibitors with significant anticoagulant activitie
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::03145f782eb525e093f927857c7919cd
https://doi.org/10.1016/j.bmcl.2007.11.019
https://doi.org/10.1016/j.bmcl.2007.11.019
Autor:
Charlene Wu, Shaila S. Shabbir, Pat M. Woollard, Alan D. Borthwick, Simon Peace, Fabrizio Nerozzi, David E. Davies, Timothy D. Westfall, John Liddle, Wendy R. Irving, Deirdre Mary Bernadette Hickey, Joanne Philp, Christopher Charles Frederick Hamlett, Derek Pollard, Mark Pullen, David P. Brooks, Gerald P. McCafferty, Richard M. Edwards, Andrew M. Mason, Steve L. Sollis, Michael Allen, Anne M. Exall
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:90-94
Optimisation of a series of oxazole diketopiperazines has led to the discovery of a very potent and selective oxytocin antagonist GSK221149A. GSK221149A has been shown to inhibit oxytocin-induced uterine contractions in the anaesthetised rat.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7169b86c2410cd3ad98037d3bf0d45c4
https://doi.org/10.1016/j.bmcl.2007.11.008
https://doi.org/10.1016/j.bmcl.2007.11.008
Autor:
Neil C. Da Costa, Alan D. Borthwick
Publikováno v:
Critical reviews in food science and nutrition. 57(4)
2,5-Diketopiperazines (2,5-DKPs) have been found to occur in a wide range of food and beverages, and display an array of chemesthetic effects (bitter, astringent, metallic, and umami) that can contribute to the taste of a variety of foods. These smal
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a6536ba64108d802e9ca6d9c959f0fd7
https://pubmed.ncbi.nlm.nih.gov/25629623
https://pubmed.ncbi.nlm.nih.gov/25629623