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Synthesis, SAR and Unanticipated Pharmacological Profiles of Analogues of the mGluR5 Ago‐potentiator ADX‐47273

descriptionPublicationkeyboard_double_arrow_right Article 09 Apr 2009 United Kingdom English Publisher:WileyJournal:ChemMedChem, volume 4, pages 505-511 (issn: 1860-7179, eissn: 1860-7187, Copyright policy )
Authors: Engers, D.W.; Rodriguez, A.L.; Williams, Richard; Hammond, A.S.; Venable, D.; Oluwatola, O.; Sulikowski, G.A.; +2 Authors

doi: 10.1002/cmdc.200800357

pmid: 19197923

pmc: PMC2865690

Synthesis, SAR and Unanticipated Pharmacological Profiles of Analogues of the mGluR5 Ago‐potentiator ADX‐47273

Abstract

AbstractAn iterative analogue library synthesis strategy rapidly developed comprehensive SAR for the mGluR5 ago‐potentiator ADX‐47273. This effort identified key substituents in the 3‐position of oxadiazole that engendered either mGluR5 ago‐potentiation or pure mGluR5 positive allosteric modulation. The mGluR5 positive allosteric modulators identified possessed the largest fold shifts (up to 27.9‐fold) of the glutamate CRC reported to date as well as providing improved physiochemical properties.magnified image

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United Kingdom
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Keywords

/dk/atira/pure/subjectarea/asjc/1300/1313, Oxadiazoles, /dk/atira/pure/subjectarea/asjc/1600/1605, Molecular Structure, Receptor, Metabotropic Glutamate 5, 610, name=Pharmacology, 540, Receptors, Metabotropic Glutamate, Structure-Activity Relationship, Toxicology and Pharmaceutics(all), name=Organic Chemistry, Piperidines, /dk/atira/pure/subjectarea/asjc/3000, name=Molecular Medicine, Combinatorial Chemistry Techniques

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selected citations
These citations are derived from selected sources.
This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Citations provided by BIP!
popularity
This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.
BIP!Popularity provided by BIP!
influence
This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Influence provided by BIP!
impulse
This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.
BIP!Impulse provided by BIP!
39
Average
Top 10%
Top 10%
bronze