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Steven Bromidge

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Fabio Maria Sabbatini; Chiara Savoia; Enzo Valerio; Filippo Visentini; Laura Zonzini; Giovanni Bernasconi; Steven M Bromidge; Mauro Corsi; Vivian J A Costantini; Lucilla D'Adamo; Carla Di Francesco; Sergio Melotto; Claudia Mundi; Elisabetta Perdonà; Benedetta Perini; Alfonso Pozzan; Marilisa Rinaldi; Romano Di Fabio
Azabicyclo[3.1.0]hexane-1-carbohydrazides as potent and selective GHSR1a ligands presenting a specific in vivo behavior.
Steven M Bromidge; Roberto Arban; Barbara Bertani; Manuela Borriello; Anna-Maria Capelli; Romano Di Fabio; Stefania Faedo; Massimo Gianotti; Laurie J Gordon; Enrica Granci; Alessandra Pasquarello; Simone K Spada; Angela Worby; Laura Zonzini; Valeria Zucchelli
5-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}-2(1H)-quinolinones and 3,4-dihydro-2(1H)-quinolinones: dual-acting 5-HT1 receptor antagonists and serotonin reuptake inhibitors. Part 3.
Steven M Bromidge; Roberto Arban; Barbara Bertani; Silvia Bison; Manuela Borriello; Paolo Cavanni; Giovanna Dal Forno; Romano Di Fabio; Daniele Donati; Stefano Fontana; Massimo Gianotti; Laurie J Gordon; Enrica Granci; Colin P Leslie; Luca Moccia; Alessandra Pasquarello; Ilaria Sartori; Anna Sava; Jeannette M Watson; Angela Worby; Laura Zonzini; Valeria Zucchelli
Design and synthesis of novel tricyclic benzoxazines as potent 5-HT(1A/B/D) receptor antagonists leading to the discovery of 6-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}-4H-imidazo[5,1-c][1,4]benzoxazine-3-carboxamide (GSK588045).

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All Publications

2011: Fabio Maria Sabbatini; Chiara Savoia; Enzo Valerio; Filippo Visentini; Laura Zonzini; Giovanni Bernasconi; Steven M Bromidge; Mauro Corsi; Vivian J A Costantini; Lucilla D'Adamo; Carla Di Francesco; Sergio Melotto; Claudia Mundi; Elisabetta Perdonà; Benedetta Perini; Alfonso Pozzan; Marilisa Rinaldi; Romano Di Fabio
Azabicyclo[3.1.0]hexane-1-carbohydrazides as potent and selective GHSR1a ligands presenting a specific in vivo behavior.
ChemMedChem 2011;6(11):1981-5.
2010: Steven M Bromidge; Roberto Arban; Barbara Bertani; Manuela Borriello; Anna-Maria Capelli; Romano Di Fabio; Stefania Faedo; Massimo Gianotti; Laurie J Gordon; Enrica Granci; Alessandra Pasquarello; Simone K Spada; Angela Worby; Laura Zonzini; Valeria Zucchelli
5-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}-2(1H)-quinolinones and 3,4-dihydro-2(1H)-quinolinones: dual-acting 5-HT1 receptor antagonists and serotonin reuptake inhibitors. Part 3.
Bioorganic & medicinal chemistry letters 2010;20(23):7092-6.
2010: Steven M Bromidge; Roberto Arban; Barbara Bertani; Silvia Bison; Manuela Borriello; Paolo Cavanni; Giovanna Dal Forno; Romano Di Fabio; Daniele Donati; Stefano Fontana; Massimo Gianotti; Laurie J Gordon; Enrica Granci; Colin P Leslie; Luca Moccia; Alessandra Pasquarello; Ilaria Sartori; Anna Sava; Jeannette M Watson; Angela Worby; Laura Zonzini; Valeria Zucchelli
Design and synthesis of novel tricyclic benzoxazines as potent 5-HT(1A/B/D) receptor antagonists leading to the discovery of 6-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}-4H-imidazo[5,1-c][1,4]benzoxazine-3-carboxamide (GSK588045).
Journal of medicinal chemistry 2010;53(15):5827-43.
2009: Steven M Bromidge; Barbara Bertani; Manuela Borriello; Andrea Bozzoli; Stefania Faedo; Massimo Gianotti; Laurie J Gordon; Matthew Hill; Valeria Zucchelli; Jeannette M Watson; Laura Zonzini
8-[2-(4-Aryl-1-piperazinyl)ethyl]-2H-1,4-benzoxazin-3(4H)-ones: dual-acting 5-HT1 receptor antagonists and serotonin reuptake inhibitors--part II.
Bioorganic & medicinal chemistry letters 2009;19(8):2338-42.
2008: Steven M Bromidge; Barbara Bertani; Manuela Borriello; Stefania Faedo; Laurie J Gordon; Enrica Granci; Matthew Hill; Howard R Marshall; Luigi P Stasi; Valeria Zucchelli; Giancarlo Merlo; Alessia Vesentini; Jeannette M Watson; Laura Zonzini
6-[2-(4-Aryl-1-piperazinyl)ethyl]-2H-1,4-benzoxazin-3(4H)-ones: dual-acting 5-HT1 receptor antagonists and serotonin reuptake inhibitors.
Bioorganic & medicinal chemistry letters 2008;18(20):5653-6.
2006: Warren D Hirst; Tania O Stean; Derek C Rogers; David Sunter; Perdita L Pugh; Stephen F Moss; Steven M Bromidge; Graham Riley; Douglas R Smith; Sarah Bartlett; Christian A Heidbreder; Alan R Atkins; laurent lacroix; Lee A Dawson; Andrew G Foley; Ciaran M Regan; Neil Upton
SB-399885 is a potent, selective 5-HT6 receptor antagonist with cognitive enhancing properties in aged rat water maze and novel object recognition models.
European journal of pharmacology 2006;553(1-3):109-19.
2006: Claire Scott; Ellen M Soffin; Matthew Hill; Peter J Atkinson; Christopher J Langmead; Paul B Wren; Stefania Faedo; Laurie J Gordon; Gary W Price; Steven M Bromidge; Christopher N Johnson; James Hagan; Jeannette Watson
SB-649915, a novel, potent 5-HT1A and 5-HT1B autoreceptor antagonist and 5-HT re-uptake inhibitor in native tissue.
European journal of pharmacology 2006;536(1-2):54-61.
2005: Caroline J Goodacre; Steven M Bromidge; David Clapham; Frank D King; Peter J Lovell; Mike Allen; Lorraine P Campbell; Vicky Holland; Graham J Riley; Kathryn R Starr; Brenda K Trail; Martyn D Wood
A series of bisaryl imidazolidin-2-ones has shown to be selective and orally active 5-HT2C receptor antagonists.
Bioorganic & medicinal chemistry letters 2005;15(22):4989-93.
2005: Mahmood Ahmed; Michael A Briggs; Steven M Bromidge; Tania Buck; Lorraine Campbell; Nigel J Deeks; Ashley Garner; Laurie Gordon; Dieter W Hamprecht; Vicky Holland; Christopher N Johnson; Andrew D Medhurst; Darren J Mitchell; Stephen F Moss; Jenifer Powles; Jon T Seal; Tania O Stean; Geoffrey Stemp; Mervyn Thompson; Brenda K Trail; Neil Upton; Kim Y Winborn; David R Witty
Bicyclic heteroarylpiperazines as selective brain penetrant 5-HT6 receptor antagonists.
Bioorganic & medicinal chemistry letters 2005;15(21):4867-71.
2005: David F Corbett; Tom D Heightman; Stephen F Moss; Steven M Bromidge; Sara A Coggon; Mark J Longley; Ana Maria Roa; Jennifer A Williams; David R Thomas
Discovery of a potent and selective 5-ht5A receptor antagonist by high-throughput chemistry.
Bioorganic & medicinal chemistry letters 2005;15(18):4014-8.
2005: Peter J Atkinson; Steven M Bromidge; Mark S Duxon; Laramie M Gaster; Michael S Hadley; Beverley Hammond; Christopher N Johnson; Derek N Middlemiss; Stephanie E North; Gary W Price; Harshad K Rami; Graham J Riley; Claire M Scott; Tracey E Shaw; Kathryn R Starr; Geoffrey Stemp; Kevin M Thewlis; David R Thomas; Mervyn Thompson; Antonio K K Vong; Jeannette M Watson
3,4-Dihydro-2H-benzoxazinones are 5-HT(1A) receptor antagonists with potent 5-HT reuptake inhibitory activity.
Bioorganic & medicinal chemistry letters 2005;15(3):737-41.
2002: Steven M Bromidge; Stephen E Clarke; Frank D King; Peter J Lovell; Helen Newman; Graham Riley; Carol Routledge; Halina T Serafinowska; Douglas R Smith; David R Thomas
Bicyclic piperazinylbenzenesulphonamides are potent and selective 5-HT6 receptor antagonists.
Bioorganic & medicinal chemistry letters 2002;12(10):1357-60.
2002: Tania O Stean; Warren D Hirst; David R Thomas; Gary W Price; Derek Rogers; Graham Riley; Steven M Bromidge; Halina T Serafinowska; Douglas R Smith; Sarah Bartlett; Nigel J Deeks; Mark S Duxon; Neil Upton
Pharmacological profile of SB-357134: a potent, selective, brain penetrant, and orally active 5-HT(6) receptor antagonist.
Pharmacology, biochemistry, and behavior 2002;71(4):645-54.
2001: Steven M Bromidge; K Griffith; T D Heightman; AJ Jennings; Frank D King; Stephen F Moss; Helen Newman; Graham Riley; Carol Routledge; Halina T Serafinowska; David R Thomas
Novel (4-piperazin-1-ylquinolin-6-yl) arylsulfonamides with high affinity and selectivity for the 5-HT(6) receptor.
Bioorganic & medicinal chemistry letters 2001;11(21):2843-6.
2001: Martyn D Wood; Charlie Reavill; Brenda K Trail; A Wilson; Tania O Stean; Guy A Kennett; S Lightowler; Thomas Blackburn; D Thomas; TL Gager; Graham Riley; Vicky Holland; Steven M Bromidge; Ian T Forbes; Derek N Middlemiss
SB-243213; a selective 5-HT2C receptor inverse agonist with improved anxiolytic profile: lack of tolerance and withdrawal anxiety.
Neuropharmacology 2001;41(2):186-99.
2001: Steven M Bromidge; Stephen E Clarke; TL Gager; K Griffith; Phillip Jeffrey; AJ Jennings; GF Joiner; Frank D King; Peter J Lovell; Stephen F Moss; Helen Newman; Graham Riley; D Rogers; Carol Routledge; Halina T Serafinowska; Douglas R Smith
Phenyl benzenesulfonamides are novel and selective 5-HT6 antagonists: identification of N-(2,5-dibromo-3-fluorophenyl)-4-methoxy-3-piperazin-1-ylbenzenesulfonamide (SB-357134).
Bioorganic & medicinal chemistry letters 2001;11(1):55-8.
2000: Steven M Bromidge; S Davies; DM Duckworth; Ian T Forbes; GE Jones; J Jones; Frank D King; Thomas Blackburn; Vicky Holland; Guy A Kennett; S Lightowler; Derek N Middlemiss; Graham J Riley; Brenda K Trail; Martyn D Wood
1-[2-[(Heteroarylmethoxy)aryl]carbamoyl]indolines are selective and orally active 5-HT2C receptor inverse agonists.
Bioorganic & medicinal chemistry letters 2000;10(16):1867-70.
2000: Steven M Bromidge; S Dabbs; S Davies; DM Duckworth; Ian T Forbes; GE Jones; J Jones; Frank D King; DV Saunders; Thomas Blackburn; Vicky Holland; Guy A Kennett; S Lightowler; Derek N Middlemiss; Graham J Riley; Brenda K Trail; Martyn D Wood
1-[2-[(Heteroaryloxy)heteroaryl]carbamoyl]indolines: novel and selective 5-HT2C receptor inverse agonists with potential as antidepressant/anxiolytic agents.
Bioorganic & medicinal chemistry letters 2000;10(16):1863-6.
2000: Carol Routledge; Steven M Bromidge; S F Moss; Gary W Price; Warren D Hirst; H Newman; Graham Riley; TL Gager; Tania O Stean; Neil Upton; S E Clarke; AM Brown; Derek N Middlemiss
Characterization of SB-271046: a potent, selective and orally active 5-HT(6) receptor antagonist.
British journal of pharmacology 2000;130(7):1606-12.
2000: Warren D Hirst; Jayne A L Minton; Steven M Bromidge; S F Moss; A J Latter; Graham Riley; Carol Routledge; Derek N Middlemiss; Gary W Price
Characterization of [(125)I]-SB-258585 binding to human recombinant and native 5-HT(6) receptors in rat, pig and human brain tissue.
British journal of pharmacology 2000;130(7):1597-605.
2000: James Hagan; Gary W Price; Phillip Jeffrey; Nigel J Deeks; Tania O Stean; DC Piper; Martin I Smith; Neil Upton; Andrew D Medhurst; Derek N Middlemiss; Graham J Riley; Peter J Lovell; Steven M Bromidge; David R Thomas
Characterization of SB-269970-A, a selective 5-HT(7) receptor antagonist.
British journal of pharmacology 2000;130(3):539-48.
2000: David R Thomas; Peter J Atkinson; M Ho; Steven M Bromidge; Peter J Lovell; A J Villani; James Hagan; Derek N Middlemiss; Gary W Price
[(3)H]-SB-269970--A selective antagonist radioligand for 5-HT(7) receptors.
British journal of pharmacology 2000;130(2):409-17.
2000: Steven M Bromidge; S Dabbs; DT Davies; S Davies; DM Duckworth; Ian T Forbes; Laramie M Gaster; P Ham; GE Jones; Frank D King; KR Mulholland; DV Saunders; Paul A Wyman; Frank E Blaney; Stephen E Clarke; Thomas Blackburn; Vicky Holland; Guy A Kennett; S Lightowler; Derek N Middlemiss; Brenda K Trail; Graham J Riley; Martyn D Wood
Biarylcarbamoylindolines are novel and selective 5-HT(2C) receptor inverse agonists: identification of 5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]- 5-pyridyl]carbamoyl]-6-trifluoromethylindoline (SB-243213) as a potential antidepressant/anxiolytic agent.
Journal of medicinal chemistry 2000;43(6):1123-34.
2000: Peter J Lovell; Steven M Bromidge; S Dabbs; DM Duckworth; Ian T Forbes; AJ Jennings; Frank D King; Derek N Middlemiss; S K Rahman; DV Saunders; L L Collin; James Hagan; Graham J Riley; David R Thomas
A novel, potent, and selective 5-HT(7) antagonist: (R)-3-(2-(2-(4-methylpiperidin-1-yl)ethyl)pyrrolidine-1-sulfonyl) phen ol (SB-269970).
Journal of medicinal chemistry 2000;43(3):342-5.
2000: Guy A Kennett; S Lightowler; Brenda K Trail; F Bright; Steven M Bromidge
Effects of RO 60 0175, a 5-HT(2C) receptor agonist, in three animal models of anxiety.
European journal of pharmacology 2000;387(2):197-204.
1999: Steven M Bromidge; S Dabbs; DT Davies; S Davies; DM Duckworth; Ian T Forbes; A Gadre; P Ham; GE Jones; Frank D King; DV Saunders; Kevin M Thewlis; D Vyas; Thomas Blackburn; Vicky Holland; Guy A Kennett; Graham J Riley; Martyn D Wood
Model studies on a synthetically facile series of N-substituted phenyl-N'-pyridin-3-yl ureas leading to 1-(3-pyridylcarbamoyl) indolines that are potent and selective 5-HT(2C/2B) receptor antagonists.
Bioorganic & medicinal chemistry 1999;7(12):2767-73.
1999: Steven M Bromidge; AM Brown; Stephen E Clarke; K Dodgson; TL Gager; H L Grassam; Phillip Jeffrey; GF Joiner; Frank D King; Derek N Middlemiss; Stephen F Moss; Helen Newman; Graham Riley; Carol Routledge; Paul A Wyman
5-Chloro-N-(4-methoxy-3-piperazin-1-yl- phenyl)-3-methyl-2-benzothiophenesulfon- amide (SB-271046): a potent, selective, and orally bioavailable 5-HT6 receptor antagonist.
Journal of medicinal chemistry 1999;42(2):202-5.
1998: Steven M Bromidge; S Dabbs; DT Davies; DM Duckworth; Ian T Forbes; P Ham; GE Jones; Frank D King; DV Saunders; S Starr; Kevin M Thewlis; Paul A Wyman; Frank E Blaney; CB Naylor; F Bailey; Thomas Blackburn; Vicky Holland; Guy A Kennett; Graham J Riley; Martyn D Wood
Novel and selective 5-HT2C/2B receptor antagonists as potential anxiolytic agents: synthesis, quantitative structure-activity relationships, and molecular modeling of substituted 1-(3-pyridylcarbamoyl)indolines.
Journal of medicinal chemistry 1998;41(10):1598-612.
1997: Steven M Bromidge; F Brown; F Cassidy; MS Clark; S Dabbs; Michael S Hadley; J Hawkins; JM Loudon; CB Naylor; Barry Orlek; Graham J Riley
Design of [R-(Z)]-(+)-alpha-(methoxyimino)-1-azabicyclo[2.2.2]octane-3-acetonitri le (SB 202026), a functionally selective azabicyclic muscarinic M1 agonist incorporating the N-methoxy imidoyl nitrile group as a novel ester bioisostere.
Journal of medicinal chemistry 1997;40(26):4265-80.
1997: JM Loudon; Steven M Bromidge; F Brown; MS Clark; Jonathan P Hatcher; J Hawkins; Graham J Riley; G Noy; Barry Orlek
SB 202026: a novel muscarinic partial agonist with functional selectivity for M1 receptors.
The Journal of pharmacology and experimental therapeutics 1997;283(3):1059-68.
1997: Steven M Bromidge; M Duckworth; Ian T Forbes; P Ham; Frank D King; Kevin M Thewlis; Frank E Blaney; CB Naylor; Thomas Blackburn; Guy A Kennett; Martyn D Wood; Stephen E Clarke
6-Chloro-5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]-5-pyridyl]carbamoyl]- indoline (SB-242084): the first selective and brain penetrant 5-HT2C receptor antagonist.
Journal of medicinal chemistry 1997;40(22):3494-6.
1997: Guy A Kennett; Martyn D Wood; F Bright; Brenda K Trail; Graham Riley; Vicky Holland; KY Avenell; Tania O Stean; Neil Upton; Steven M Bromidge; Ian T Forbes; AM Brown; Derek N Middlemiss; Thomas Blackburn
SB 242084, a selective and brain penetrant 5-HT2C receptor antagonist.
Neuropharmacology 1997;36(4-5):609-20.
1992: S M Jenkins; H J Wadsworth; Steven M Bromidge; Barry Orlek; Paul A Wyman; Graham J Riley; J Hawkins
Substituent variation in azabicyclic triazole- and tetrazole-based muscarinic receptor ligands.
Journal of medicinal chemistry 1992;35(13):2392-406.