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Gerard Giblin

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Mairi Sime; Timothy M Wilson; Robert X Xu; Timothy M Willson; Amanda C Allan; Paul Chapman; Charlotte Fieldhouse; Gerard M P Giblin; Mark P Healy; Millard H Lambert; Lisa M Leesnitzer; Ann Lewis; Raymond V Merrihew; Richard A Rutter; Rosemary Sasse; Barry G Shearer; David J Virley
Discovery of GSK1997132B a novel centrally penetrant benzimidazole PPARγ partial agonist.
Amanda C Allan; Andy Billinton; Susan H Brown; Anita Chowdhury; Andrew J Eatherton; Charlotte Fieldhouse; Gerard M P Giblin; Paul Goldsmith; Adrian Hall; David N Hurst; Alan Naylor; D Anthony Rawlings; Tiziana Scoccitti; Mairi Sime; Pamela J Theobald
Discovery of a novel series of nonacidic benzofuran EP1 receptor antagonists.
Ishrut Hussain; David C Harrison; Julie Hawkins; Trevor Chapman; Ian Marshall; Laura Facci; Sharlin Ahmed; Kim Brackenborough; Stephen Skaper; Tania L Mead; Beverley B Smith; Gerard M P Giblin; Adrian Hall; M Isabel Gonzalez; Jill C Richardson
TASTPM mice expressing amyloid precursor protein and presenilin-1 mutant transgenes are sensitive to γ-secretase modulation and amyloid-β₄₂ lowering by GSM-10h.

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All Publications

2011: Mairi Sime; Timothy M Wilson; Robert X Xu; Timothy M Willson; Amanda C Allan; Paul Chapman; Charlotte Fieldhouse; Gerard M P Giblin; Mark P Healy; Millard H Lambert; Lisa M Leesnitzer; Ann Lewis; Raymond V Merrihew; Richard A Rutter; Rosemary Sasse; Barry G Shearer; David J Virley
Discovery of GSK1997132B a novel centrally penetrant benzimidazole PPARγ partial agonist.
Bioorganic & medicinal chemistry letters 2011;21(18):5568-72.
2011: Amanda C Allan; Andy Billinton; Susan H Brown; Anita Chowdhury; Andrew J Eatherton; Charlotte Fieldhouse; Gerard M P Giblin; Paul Goldsmith; Adrian Hall; David N Hurst; Alan Naylor; D Anthony Rawlings; Tiziana Scoccitti; Mairi Sime; Pamela J Theobald
Discovery of a novel series of nonacidic benzofuran EP1 receptor antagonists.
Bioorganic & medicinal chemistry letters 2011;21(14):4343-8.
2011: Ishrut Hussain; David C Harrison; Julie Hawkins; Trevor Chapman; Ian Marshall; Laura Facci; Sharlin Ahmed; Kim Brackenborough; Stephen Skaper; Tania L Mead; Beverley B Smith; Gerard M P Giblin; Adrian Hall; M Isabel Gonzalez; Jill C Richardson
TASTPM mice expressing amyloid precursor protein and presenilin-1 mutant transgenes are sensitive to γ-secretase modulation and amyloid-β₄₂ lowering by GSM-10h.
Neuro-degenerative diseases 2011;8(1-2):15-24.
2010: Adrian Hall; Richard L Elliott; Gerard M P Giblin; Ishrut Hussain; James Musgrave; Alan Naylor; Rosemary Sasse; Beverley Smith
Piperidine-derived gamma-secretase modulators.
Bioorganic & medicinal chemistry letters 2010;20(3):1306-11.
2010: Robert J Gleave; Paul J Beswick; Andrew J Brown; Gerard M P Giblin; Paul Goldsmith; Carl P Haslam; William L Mitchell; Neville H Nicholson; Lee W Page; Sadhana Patel; Susan Roomans; Brian P Slingsby; Martin E Swarbrick
Synthesis and evaluation of 3-amino-6-aryl-pyridazines as selective CB(2) agonists for the treatment of inflammatory pain.
Bioorganic & medicinal chemistry letters 2010;20(2):465-8.
2009: Robert J Gleave; Paul J Beswick; Andrew J Brown; Gerard M P Giblin; Carl P Haslam; David Livermore; Andrew Moses; Neville H Nicholson; Lee W Page; Brian Slingsby; Martin E Swarbrick
2-Amino-5-aryl-pyridines as selective CB2 agonists: synthesis and investigation of structure-activity relationships.
Bioorganic & medicinal chemistry letters 2009;19(23):6578-81.
2009: Gerard M P Giblin; Andrew Billinton; Michael Briggs; Andrew J Brown; Iain P Chessell; Nick M Clayton; Andrew J Eatherton; Paul Goldsmith; Carl Haslam; Matthew R Johnson; William L Mitchell; Alan Naylor; Alcide Perboni; Brian P Slingsby; Alex W Wilson
Discovery of 1-[4-(3-chlorophenylamino)-1-methyl-1H-pyrrolo[3,2-c]pyridin-7-yl]-1-morpholin-4-ylmethanone (GSK554418A), a brain penetrant 5-azaindole CB2 agonist for the treatment of chronic pain.
Journal of medicinal chemistry 2009;52(19):5785-8.
2009: Adrian Hall; Andy Billinton; Susan H Brown; Anita Chowdhury; Nicholas M Clayton; Gerard M P Giblin; Mairi Gibson; Paul A Goldsmith; David N Hurst; Alan Naylor; Caroline F Peet; Tiziana Scoccitti; Alexander W Wilson; Wendy Winchester
Discovery of sodium 6-[(5-chloro-2-{[(4-chloro-2-fluorophenyl)methyl]oxy}phenyl)methyl]-2-pyridinecarboxylate (GSK269984A) an EP(1) receptor antagonist for the treatment of inflammatory pain.
Bioorganic & medicinal chemistry letters 2009;19(9):2599-603.
2009: Adrian Hall; Susan H Brown; Christopher Budd; Nicholas M Clayton; Gerard M P Giblin; Paul Goldsmith; Thomas G Hayhow; David N Hurst; Alan Naylor; D Anthony Rawlings; Tiziana Scoccitti; Alexander W Wilson; Wendy J Winchester
Discovery of GSK345931A: An EP(1) receptor antagonist with efficacy in preclinical models of inflammatory pain.
Bioorganic & medicinal chemistry letters 2009;19(2):497-501.
2009: William L Mitchell; Gerard M P Giblin; Alan Naylor; Andrew J Eatherton; Brian P Slingsby; Anthony D Rawlings; Karamjit S Jandu; Carl P Haslam; Andrew J Brown; Paul Goldsmith; Nick M Clayton; Alex W Wilson; Iain P Chessell; Richard H Green; Andrew R Whittington; Ian D Wall
Pyridine-3-carboxamides as novel CB(2) agonists for analgesia.
Bioorganic & medicinal chemistry letters 2009;19(1):259-63.
2008: Adrian Hall; Andy Billinton; Alan K Bristow; Susan H Brown; Anita Chowdhury; Leanne Cutler; Gerard M P Giblin; Paul Goldsmith; Thomas G Hayhow; Ian R Kilford; Alan Naylor; Barry Passingham; D Anthony Rawlings
Discovery of brain penetrant, soluble, pyrazole amide EP1 receptor antagonists.
Bioorganic & medicinal chemistry letters 2008;18(14):4027-32.
2008: Adrian Hall; Andy Billinton; Susan H Brown; Nicholas M Clayton; Anita Chowdhury; Gerard M P Giblin; Paul Goldsmith; Thomas G Hayhow; David N Hurst; Ian R Kilford; Alan Naylor; Barry Passingham; Lisa Winyard
Non-acidic pyrazole EP1 receptor antagonists with in vivo analgesic efficacy.
Bioorganic & medicinal chemistry letters 2008;18(11):3392-9.
2008: Adrian Hall; Andy Billinton; Susan H Brown; Anita Chowdhury; Gerard M P Giblin; Paul Goldsmith; David N Hurst; Alan Naylor; Sadhana Patel; Tiziana Scoccitti; Pamela J Theobald
Discovery of a novel indole series of EP1 receptor antagonists by scaffold hopping.
Bioorganic & medicinal chemistry letters 2008;18(8):2684-90.
2008: Adrian Hall; Rino A Bit; Susan H Brown; Anita Chowdhury; Gerard M P Giblin; David N Hurst; Ian R Kilford; Xiao Lewell; Alan Naylor; Tiziana Scoccitti
Novel methylene-linked heterocyclic EP1 receptor antagonists.
Bioorganic & medicinal chemistry letters 2008;18(5):1592-7.
2007: Adrian Hall; Andy Billinton; Gerard M P Giblin
EP1 antagonists for the treatment of inflammatory pain.
Current opinion in drug discovery & development 2007;10(5):597-612.
2007: Adrian Hall; Susan H Brown; Anita Chowdhury; Gerard M P Giblin; Mairi Gibson; Mark P Healy; David G Livermore; Richard J Wilson; Alan Naylor; D Anthony Rawlings; Shilina Roman; Emma Ward; Caroline Willay
Identification and optimization of novel 1,3,4-oxadiazole EP1 receptor antagonists.
Bioorganic & medicinal chemistry letters 2007;17(16):4450-5.
2007: Gerard M P Giblin; Celestine T O'Shaughnessy; Alan Naylor; William L Mitchell; Andrew J Eatherton; Brian P Slingsby; D Anthony Rawlings; Paul Goldsmith; Andrew J Brown; Claudine Haslam; Nicholas M Clayton; Alex W Wilson; Iain P Chessell; Andrew R Wittington; Richard Green
Discovery of 2-[(2,4-dichlorophenyl)amino]-N-[(tetrahydro- 2H-pyran-4-yl)methyl]-4-(trifluoromethyl)- 5-pyrimidinecarboxamide, a selective CB2 receptor agonist for the treatment of inflammatory pain.
Journal of medicinal chemistry 2007;50(11):2597-600.
2007: Stephen C McKeown; Adrian Hall; Richard Blunt; Susan H Brown; Iain P Chessell; Anita Chowdhury; Gerard M P Giblin; Mark P Healy; Matthew R Johnson; Olivier Lorthioir; Anton D Michel; Alan Naylor; Xiao Q Lewell; Shilina Roman; Stephen P Watson; Wendy J Winchester; Richard J Wilson
Identification of novel glycine sulfonamide antagonists for the EP1 receptor.
Bioorganic & medicinal chemistry letters 2007;17(6):1750-4.
2007: Adrian Hall; Stephen Atkinson; Susan H Brown; Iain P Chessell; Anita Chowdhury; Gerard M P Giblin; Paul Goldsmith; Mark P Healy; Karamjit S Jandu; Matthew R Johnson; Anton D Michel; Alan Naylor; Jennifer Sweeting
Discovery of novel, non-acidic 1,5-biaryl pyrrole EP1 receptor antagonists.
Bioorganic & medicinal chemistry letters 2007;17(5):1200-5.
2007: Adrian Hall; Susan H Brown; Iain P Chessell; Anita Chowdhury; Nicholas M Clayton; Tanya Coleman; Gerard M P Giblin; Beverley Hammond; Mark P Healy; Matthew R Johnson; Ann Metcalf; Anton D Michel; Alan Naylor; Riccardo Novelli; David J Spalding; Jennifer Sweeting; Lisa A Winyard
1,5-Biaryl pyrrole derivatives as EP1 receptor antagonists. Structure-activity relationships of 6-substituted and 5,6-disubstituted benzoic acid derivatives.
Bioorganic & medicinal chemistry letters 2007;17(4):916-20.
2007: Adrian Hall; Susan H Brown; Iain P Chessell; Anita Chowdhury; Nicholas M Clayton; Tanya Coleman; Gerard M P Giblin; Beverley Hammond; Mark P Healy; Matthew R Johnson; Ann Metcalf; Anton D Michel; Alan Naylor; Riccardo Novelli; David J Spalding; Jennifer Sweeting
1,5-Biaryl pyrrole derivatives as EP1 receptor antagonists: Structure-activity relationships of 4- and 5-substituted benzoic acid derivatives.
Bioorganic & medicinal chemistry letters 2007;17(3):732-5.
2007: Gerard M P Giblin; Rino A Bit; Susan H Brown; Helene Chaignot; Anita Chowdhury; Iain P Chessell; Nicholas M Clayton; Tanya Coleman; Adrian Hall; Beverley Hammond; David N Hurst; Anton D Michel; Alan Naylor; Riccardo Novelli; Tiziana Scoccitti; David J Spalding; Sac P Tang; Alex W Wilson; Rich Wilson
The discovery of 6-[2-(5-chloro-2-{[(2,4-difluorophenyl)methyl]oxy}phenyl)-1-cyclopenten-1-yl]-2-pyridinecarboxylic acid, GW848687X, a potent and selective prostaglandin EP1 receptor antagonist for the treatment of inflammatory pain.
Bioorganic & medicinal chemistry letters 2007;17(2):385-9.
2006: Stephen C McKeown; Adrian Hall; Gerard M P Giblin; Olivier Lorthioir; Richard Blunt; Xiao Q Lewell; Richard J Wilson; Susan H Brown; Anita Chowdhury; Tanya Coleman; Stephen P Watson; Iain P Chessell; Adrian Pipe; Nick Clayton; Paul Goldsmith
Identification of novel pyrazole acid antagonists for the EP1 receptor.
Bioorganic & medicinal chemistry letters 2006;16(18):4767-71.
2006: Adrian Hall; Stephen Atkinson; Susan H Brown; Iain P Chessell; Anita Chowdhury; Nicholas M Clayton; Tanya Coleman; Gerard M P Giblin; Robert J Gleave; Beverley Hammond; Mark P Healy; Matthew R Johnson; Anton D Michel; Alan Naylor; Riccardo Novelli; David J Spalding; Sac P Tang
Structure-activity relationships of 1,5-biaryl pyrroles as EP1 receptor antagonists.
Bioorganic & medicinal chemistry letters 2006;16(14):3657-62.
2006: Richard J Wilson; Gerard M P Giblin; Susan Roomans; Sharron A Rhodes; Kerri-Ann Cartwright; Vanessa J Shield; Jason Brown; Alan Wise; Jannatara Chowdhury; Sara Pritchard; Jim Coote; Lloyd S Noel; Terry Kenakin; Cynthia L Burns-Kurtis; Valerie Morrison; David W Gray; Heather Giles
GW627368X ((N-{2-[4-(4,9-diethoxy-1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl)phenyl]acetyl} benzene sulphonamide): a novel, potent and selective prostanoid EP4 receptor antagonist.
British journal of pharmacology 2006;148(3):326-39.
2006: Adrian Hall; Rino A Bit; Susan H Brown; Helene Chaignot; Iain P Chessell; Tanya Coleman; Gerard M P Giblin; David N Hurst; Ian R Kilford; Xiao Q Lewell; Anton D Michel; Shiyam Mohamed; Alan Naylor; Riccardo Novelli; Lee Skinner; David J Spalding; Sac P Tang; Richard J Wilson
Discovery of novel biaryl heterocyclic EP1 receptor antagonists.
Bioorganic & medicinal chemistry letters 2006;16(10):2666-71.
2005: Jonathan Foot; Gerard M P Giblin; Adrian C Whitwood; Richard J K Taylor
Unexpected Z-stereoselectivity in the Ramberg-Bäcklund reaction of diarylsulfones leading to cis-stilbenes: the effect of aryl substituents and application in the synthesis of the integrastatin nucleus.
Organic & biomolecular chemistry 2005;3(5):756-63.
2003: Jonathan Foot; Gerard M P Giblin; Richard J K Taylor
Synthesis of the integrastatin nucleus using the Ramberg-Bäcklund reaction.
Organic letters 2003;5(23):4441-4.
2003: Gerard M P Giblin; Douglas T Kirk; Lee Mitchell; Nigel S Simpkins
Bridgehead enolates: substitution and asymmetric desymmetrization of small bridged carbonyl compounds by lithium amide bases.
Organic letters 2003;5(10):1673-5.
2001: Gerard M P Giblin; P C Box; I B Campbell; A P Hancock; S Roomans; G I Mills; C Molloy; G E Tranter; A L Walker; Susan R Doctrow; Karl Huffman; Bernard Malfroy
6,6'-Bis(2-hydroxyphenyl)-2,2'-bipyridine manganese(III) complexes: a novel series of superoxide dismutase and catalase mimetics.
Bioorganic & medicinal chemistry letters 2001;11(11):1367-70.