Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1374334 | Bioorganic & Medicinal Chemistry Letters | 2011 | 5 Pages |
Abstract
Based on SAR in the alkyne class of mGlu5 receptor negative allosteric modulators and a set of amide-based positive allosteric modulators, optimized substitution of the aryl ‘b’ ring was used to create substituted N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides. Results from an mGlu5 receptor functional assay, using calcium fluorescence, revealed varying efficacies and potencies that provide evidence that subtle changes in compounds within a close structural class can have marked effects on functional activity including switches in modes of efficacy (i.e., negative to positive allosteric modulation).
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Mu-Fa Zou, Jianjing Cao, Alice L. Rodriguez, P. Jeffrey Conn, Amy Hauck Newman,