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Bioorg Med Chem Lett. 2011 May 1;21(9):2650-4. doi: 10.1016/j.bmcl.2010.12.110. Epub 2010 Dec 28.

Design and synthesis of substituted N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides as positive allosteric modulators of the metabotropic glutamate receptor subtype 5.

Author information

1
Medicinal Chemistry Section, National Institute on Drug Abuse-Intramural Research Program, National Institutes of Health, 333 Cassell Drive Baltimore, MD 21224, USA.

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).

PMID:
21295978
PMCID:
PMC3081927
DOI:
10.1016/j.bmcl.2010.12.110
[Indexed for MEDLINE]
Free PMC Article

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