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The Synthesis and Use of Certain Pyridine Derivatives as Modulators of the G-protein Coupled Receptors mGlu5 and P2Y12


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Title: The Synthesis and Use of Certain Pyridine Derivatives as Modulators of the G-protein Coupled Receptors mGlu5 and P2Y12
Authors: Bach, Peter
E-mail: bach@chalmers.se
Issue Date: 20-Nov-2012
University: University of Gothenburg. Faculty of Science
Institution: Department of Chemistry ; Institutionen för kemi
Parts of work: I Bach, P.; Nilsson, K.; Wållberg, A.; Bauer, U.; Hammerland, L. G.; Peterson, A.; Svensson, T.; Österlund, K.; Karis, D.; Boije, M; Wensbo, D. A New Series of Pyridinyl-alkynes as Antagonists of the Metabotropic Glutamate Receptor 5 (mGluR5). Bioorg. Med. Chem. Lett. 2006, 16, 4792-4795.
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II Bach, P.; Nilsson, K.; Svensson, T.; Bauer, U.; Hammerland, L. G.; Peterson, A.; Wållberg, A.; Österlund, K.; Karis, D.; Boije, M; Wensbo, D. “Structure-activity Relationships for the Linker in a Series of Pyridinyl-alkynes that are Antagonists of the Metabotropic Glutamate Receptor 5 (mGluR5). Bioorg. Med. Chem. Lett. 2006, 16, 4788-4791.
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III Bach, P. Boström, J.; Brickmann, K.; van Giezen, J. J. J.; Hovland, R.; Petersson, A. U.; Ray, A.; Zetterberg, F. A Novel Series of Piperazinyl-pyridine Ureas as Antagonists of the Purinergic P2Y12 Receptor. Bioorg. Med. Chem. Lett. 2011, 21, 2877-2881.
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IV Bach, P.; Boström, J.; Brickmann, K.; van Giezen, J. J. J.; Groneberg, R. D.; Harvey, D. M.; O’Sullivan, M.; Zetterberg, F. Synthesis, Structure-Property Relationships and Pharmacokinetic Evaluation of Ethyl 6-Aminonicotinate Sulfonylureas as Antagonists of the P2Y12 Receptor. Manuscript.

V Bach, P.; Boström, J.; Brickmann, K.; Burgess, L. E.; Clarke, D.; Groneberg, R. D.; Harvey, D. M.; Groneberg, R. D.; Harvey, D. M.; Laird, E. R.; O’Sullivan, M.; Zetterberg, F. 5-Alkyl-1,3-oxazole Derivatives of 6-Amino-nicotinic Acids as Alkyl Ester Bioisosteres are Antagonists of the P2Y12 Receptor. Submitted.

VI Bach, P.; Marczynke, M.; Giordanetto, F. Effects of the Pyridine 3-Substituent on the Regioselectivity in the Nucleophilic Aromatic Substitution Reaction of 3-Substituted 2,6-Dichloropyridines with 1-Methylpiperazine Studied by a Chemical Design Strategy. Eur. J. Org. Chem. Accepted.
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Date of Defence: 2012-12-12
Disputation: Onsdagen den 12. december 2012, Föreläsningssal HA3, Hörsalsvägen 4, Göteborgs Universitet.
Degree: Doctor of Philosophy
Publication type: Doctoral thesis
Keywords: mGluR5, P2Y12, gastroesophageal reflux disease (GERD), thrombosis, ethyl nicotinates, ureas, sulfonylureas, oxazoles, bioisosteres, regioselectivity, solvent effect.
Abstract: The glutamatergic mGlu5 receptor and the purinergic P2Y12 receptor are two important targets in the development of novel treatments of gastroesophageal reflux disease (GERD) and thrombosis, respectively. Synthesis was developed to investigate the structure-activity relationships (SAR) of a novel series of 2-alkynylpyridine derivatives as mGluR5 antagonists. This led to the discovery of antagonists with potency in the low-nanomolar range. High microsomal metabolism, possibly due to high lipop... more
ISBN: 978-91-628-8579-3
URI: http://hdl.handle.net/2077/30683
Appears in Collections:Doctoral Theses from University of Gothenburg / Doktorsavhandlingar från Göteborgs universitet
Doctoral Theses / Doktorsavhandlingar Institutionen för kemi och molekylärbiologi

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