Zobrazeno 1 - 10
of 58
pro vyhledávání: '"Jeannette M. Watson"'
Autor:
Barry V. O'Neill, Pradeep J. Nathan, Jon Robertson, Gareth A. Jones, Jesper Lund, Stephen P. Watson, Gary Peters, Marc Laruelle, Ceri H. Davies, Rodney J. Croft, Jeannette M. Watson, Philip Lawrence, Paul Maruff, Chris M. Dodds, Edward T. Bullmore, Graham D Bentley, Bridget Swirski
Publikováno v:
International Journal of Neuropsychopharmacology. 16:721-731
Episodic memory deficits are a core feature of neurodegenerative disorders. Muscarinic M1 receptors play a critical role in modulating learning and memory and are highly expressed in the hippocampus. We examined the effect of GSK1034702, a potent M1
Autor:
Jim J. Hagan, Claire M. Scott, Jeannette M. Watson, Kathryn R. Starr, Zoe A. Hughes, Trevor Sharp, Michael J. Newson, Lee A. Dawson
RATIONALE: The delay in onset and treatment resistance of subpopulations of depressed patients to conventional serotonin reuptake inhibitors has lead to new drug development strategies to produce agents with improved antidepressant efficacy. OBJECTIV
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6725de5da20a0659e2eba1f53cdc2273
https://doi.org/10.1007/s00213-006-0691-x
https://doi.org/10.1007/s00213-006-0691-x
Autor:
Neil Upton, Tania O. Stean, Claire Roberts, Michael S. Hadley, Vicky Holland, Gary W. Price, Laurie J. Gordon, Jeannette M. Watson, Jenifer Powles, Claire M. Scott, Leanne Cutler, Tanya Coleman, Tom D. Heightman, Andrew Ayrton, Jean-Pierre Pilleux, Sarah L. Pardoe, Graham J. Riley, Laramie Mary Gaster, Nigel E. Austin, Brenda K. Trail, Derek N. Middlemiss
The novel 8-piperazinyl-2,3-dihydropyrroloisoquinoline template was synthesized in nine steps. The template was N-substituted to give a series of compounds showing binding to human cloned 5-HT1A, 5-HT1B and 5-HT1D receptors with pKi’s greater than
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::86421f00e16772e71fb543436a7895c9
https://doi.org/10.1016/j.bmcl.2005.06.042
https://doi.org/10.1016/j.bmcl.2005.06.042
Publikováno v:
Targets and Emerging Therapies for Schizophrenia
Autor:
Paul W. Smith, Ian Thomson Forbes, Andrea M. Bradford, Graham Walker, Graham Murkitt, Wyman Paul Adrian, Graeme Irvine Stevenson, Dale James Johnson, Jeannette M. Watson, Steve P. Watson, Adam J. Lucas, Claudette Mookherjee, Fiona Brown, Vincenzo Garzya, Sean Thomas Flynn, Jane Gartlon, Harminder Mudhar
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:5434-5438
A series of N-substituted 3-(4-piperidinyl)-1,3-benzoxazolinones and oxindoles are reported which were found to be potent and selective muscarinic M 1 agonists. By control of the physicochemical characteristics of the series, particularly the lipophi
Autor:
Ilaria Sartori, Laura Zonzini, Laurie J. Gordon, Angela Worby, Stefano Fontana, Manuela Borriello, Silvia Bison, Jeannette M. Watson, Steven Mark Bromidge, Giovanna Dal Forno, Colin Philip Leslie, Alessandra Pasquarello, Anna Sava, Luca G. Moccia, Barbara Bertani, Roberto Arban, Daniele Donati, Enrica Granci, Valeria Zucchelli, Paolo Cavanni, Massimo Gianotti, Romano Di-Fabio
Publikováno v:
Journal of Medicinal Chemistry. 53:5827-5843
Bioisoteric replacement of the metabolically labile N-methyl amide group of a series of benzoxazinones with small heterocyclic rings has led to novel series of fused tricyclic benzoxazines which are potent 5-HT1A/B/D receptor antagonists with and wit
Autor:
Christopher J. Langmead, Vincenzo Garzya, Joanne Pardoe, Ralph A. Rivero, Jeannette M. Watson, Ben Tehan, Ian Thomson Forbes, Jian Jin, Adam J. Lucas, Dongchuan Shi, Marie Woolley-Roberts, Zining Wu, Brian Budzik, Graham Walker
Publikováno v:
ACS Medicinal Chemistry Letters. 1:244-248
Virtual screening of the corporate compound collection yielded compound 1 as a subtype selective muscarinic M1 receptor agonist hit. Initial optimization of the N-capping group of the central piperidine ring resulted in compounds 2 and 3 with signifi
Autor:
Christopher J. Langmead, Dongchuan Shi, Graham Walker, Yann Lauchart, Jeannette M. Watson, Jian Jin, Zining Wu, Adam J. Lucas, Vincenzo Garzya, Ralph A. Rivero, Ian Thomson Forbes, Brian Budzik
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:3545-3549
Further optimization of the biaryl amide series via extensively exploring structure–activity relationships resulted in potent and subtype selective M1 agonists exemplified by compounds 9a and 9j with good rat PK properties including CNS penetration
Autor:
Vimesh Ashvinkumar Avlani, Patrick M. Sexton, Benjamin G. Tehan, Elizabeth Guida, Arthur Christopoulos, Christopher J. Langmead, Martyn D. Wood, Hugh J. Herdon, Jeannette M. Watson
Publikováno v:
Molecular Pharmacology. 78:94-104
Recent years have witnessed the discovery of novel selective agonists of the M(1) muscarinic acetylcholine (ACh) receptor (mAChR). One mechanism invoked to account for the selectivity of such agents is that they interact with allosteric sites. We inv
Autor:
Jeannette M. Watson, Simon E. Ward
Publikováno v:
Current Topics in Medicinal Chemistry. 10:479-492
This article highlights recent advances in the discovery of new agonists, antagonists and partial agonists of the 5-HT(1D) receptor. The field of 5-HT(1D) agonists continues to deliver a number of new potential therapeutic agents, although advances i