Zobrazeno 1 - 10
of 13
pro vyhledávání: '"Patrick M. Woollard"'
Autor:
Fabrizio Nerozzi, Shalia S Shabbir, Paul G. Wyatt, Mamta Patel, Michael Allen, Josie Chilcott, Christopher J. Gardner, Marion J. Perren, Jackie E. Mordaunt, Livermore David, Gordon G. Weingarten, Ping Zhou, Patrick M. Woollard
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 12:1405-1411
The paper covers continuing efforts to discover novel, potent and selective oxytocin antagonists. Further benzofuran derivatives with potent oxytocin antagonist activity and good pharmacokinetic parameters are reported. Efforts to improve the in vivo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3e1b65e9e762608b3da232e63c0d7e45
https://doi.org/10.1016/s0960-894x(02)00160-9
https://doi.org/10.1016/s0960-894x(02)00160-9
Autor:
Josie Chilcott, Paul Wyatt, Alison Foster, Jan Scicinski, Livermore David, Patrick M. Woollard, Michael J. Allen, Jackie E. Mordaunt
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 12:1399-1404
Studies to discover novel, potent and selective oxytocin antagonists are reported. Combinatorial libraries designed to find novel replacements of fragments of oxytocin antagonist L-371,257, identified pyrimidine, thiazole, indole and benzofuran as po
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::11967548f9f2b9d5d19dcd0b66893618
https://doi.org/10.1016/s0960-894x(02)00159-2
https://doi.org/10.1016/s0960-894x(02)00159-2
Autor:
Patrick M. Woollard, Anne M. Exall, Deirdre Mary Bernadette Hickey, Fabrizio Nerozzi, Ian Edward David Smith, John Liddle, Dave E. Davies, Simon Peace, Timothy D. Westfall, Mark Pullen, Michael Allen, Alan D. Borthwick, Andrew M. Mason, Dinesh Stanislaus, Steve L. Sollis, Christopher Charles Frederick Hamlett, Derek Pollard
Publikováno v:
Journal of medicinal chemistry. 55(2)
A six-stage stereoselective synthesis of indanyl-7-(3'-pyridyl)-(3R,6R,7R)-2,5-diketopiperazines oxytocin antagonists from indene is described. SAR studies involving mono- and disubstitution in the 3'-pyridyl ring and variation of the 3-isobutyl grou
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fb0105f246aa79833007ec247c9dd297
https://pubmed.ncbi.nlm.nih.gov/22239250
https://pubmed.ncbi.nlm.nih.gov/22239250
Autor:
Elisa Ballini, Benjamin D. Bax, Beatrice Oliosi, Claudette Mookherjee, Daniel Marcus Bradley, Stuart P. Ballantine, Nigel E. Austin, Kevin M. Thewlis, Rosemary A. Melarange, Shahnaz P. Yusaf, Gianni Dal Negro, Andrew Jonathan Harris, J. Mosley, Kathrine J. Smith, Laura Aldegheri, Simon E. Ward, B. Clarke, Stephen A Harrison, Mark H Harries, Patrick M. Woollard
Publikováno v:
Journal of medicinal chemistry. 54(1)
A novel series of AMPAR positive modulators is described that were identified by high throughput screening. The molecules of the series have been optimized from a high quality starting point hit to afford excellent developability, tolerability, and e
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5f968ae85bfba5e74967880d1ee4d863
https://pubmed.ncbi.nlm.nih.gov/21128618
https://pubmed.ncbi.nlm.nih.gov/21128618
Autor:
Jackie E. Mordaunt, Paul Wyatt, Michael J. Allen, Alison Foster, Livermore David, Jan Scicinski, Josie Chilcott, Patrick M. Woollard
Publikováno v:
ChemInform. 33
Studies to discover novel, potent and selective oxytocin antagonists are reported. Combinatorial libraries designed to find novel replacements of fragments of oxytocin antagonist L-371,257, identified pyrimidine, thiazole, indole and benzofuran as po
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::955cc0b1469ba5adf5d66c959e356c2a
https://doi.org/10.1002/chin.200236159
https://doi.org/10.1002/chin.200236159
Autor:
Martyn D. Wood, Daniele Donati, Steve P. Watson, Claire M. Howes, Payne Andrew H, Patrick M. Woollard, Silvia Terreni, Romano Di Fabio, Ian Peter Holmes, Charlie Reavill, Andy Gribble, Angela Worby, Richard Blunt, Luca Arista, Stephen M. Blowers, Olivier Lorthioir, Dieter Hamprecht, Ian Stansfield, Fabrizio Micheli
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(6)
The identification of a highly selective D 2 partial agonist, D 3 antagonist tool molecule which demonstrates high levels of brain exposure and selectivity against an extensive range of dopamine, serotonin, adrenergic, histamine, and muscarinic recep
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::53d0ba34865e65682eabe24ee8d42e85
https://pubmed.ncbi.nlm.nih.gov/20153647
https://pubmed.ncbi.nlm.nih.gov/20153647
Autor:
Patrick M. Woollard, Charlene Wu, Mark Pullen, Michael Allen, Richard M. Edwards, David P. Brooks, Deirdre Mary Bernadette Hickey, John Liddle, Gerald P. McCafferty, Alan D. Borthwick, Timothy D. Westfall
Publikováno v:
American journal of physiology. Regulatory, integrative and comparative physiology. 293(1)
Spontaneous and induced uterine contractions in the rat were found to be inhibited by a novel and selective oxytocin receptor antagonist GSK221149A (3 R,6 R)-3-Indan-2-yl-1-[(1 R)-1-(2-methyl-1,3-oxazol-4-yl)-2-morpholin-4-yl-2-oxoethyl]-6-[(1 S)-1-m
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::773b59f827d4637cc59221fcc48ac895
https://pubmed.ncbi.nlm.nih.gov/17395790
https://pubmed.ncbi.nlm.nih.gov/17395790
Autor:
Alan D. Borthwick, Dave E. Davies, Anne M. Exall, Richard J. D. Hatley, Jennifer A. Hughes, Wendy R. Irving, David G. Livermore, Steve L. Sollis, Fabrizio Nerozzi, Klara L. Valko, Michael J. Allen, Marion Perren, Shalia S. Shabbir, Patrick M. Woollard, Mark A. Price
Publikováno v:
Journal of medicinal chemistry. 49(14)
A short, efficient, and highly stereoselective synthesis of a series of (3R,6R,7R)-2,5-diketopiperazine oxytocin antagonists and their pharmacokinetics in rat and dog is described. Prediction of the estimated human oral absorption (EHOA) using measur
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ff9f99084e0ca4f2c727fbd23a0eaf80
https://pubmed.ncbi.nlm.nih.gov/16821776
https://pubmed.ncbi.nlm.nih.gov/16821776
Autor:
Marion J. Perren, Michael Allen, Patrick M. Woollard, Alan D. Borthwick, Paul G. Wyatt, Anne M. Exall, Dave E. Davies, Shalia S Shabbir, Steve L. Sollis, Fabrizio Nerozzi, Livermore David
Publikováno v:
Journal of medicinal chemistry. 48(22)
A short stereoselective synthesis of a series of chiral 7-aryl-2,5-diketopiperazines oxytocin antagonists is described. Varying the functionality and substitution pattern of substituents in the 7-aryl ring and varying the chirality of this exocyclic
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::248d5a4c254ef2deee7352b8c047c9c7
https://pubmed.ncbi.nlm.nih.gov/16250654
https://pubmed.ncbi.nlm.nih.gov/16250654
Autor:
Neil Derek Miller, Paul G. Wyatt, Josie Chilcott, Gwen Hickin, Patrick M. Woollard, Michael Allen
Publikováno v:
Bioorganicmedicinal chemistry letters. 11(10)
We have investigated the structure-activity relationships of the 1- and 3-substituents and replacements of the 5-phenyl group of GW405212X 1, a potent selective oxytocin antagonist. The effect of these modifications on oxytocin binding antagonism and
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::de1f8ac55e70ea4b2078b792ea933668
https://pubmed.ncbi.nlm.nih.gov/11392542
https://pubmed.ncbi.nlm.nih.gov/11392542