Synthesis and biological activity of allosteric modulators of GABA B receptors part 3. 3-(2,6-bis-iso-propyl-4-hydroxyphenyl)propanols

doi:10.1590/S0103-50532007000400009

Paper

Synthesis and biological activity of allosteric modulators of GABA B receptors part 3. 3-(2,6-bis-iso-propyl-4-hydroxyphenyl)propanols

Published 2007 · D. Kerr, J. Khalafy, J. Ong

Journal of the Brazilian Chemical Society

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3

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Abstract

A series of six 2,2-disubstituted 3-[3,5-di-iso-propyl-4-hydroxyphenyl]propan-1-ol derivatives have been prepared for evaluation as allosteric modulators of GABAB receptors. The activity (EC50 30 µM) was greatest for the dimethyl analogue, but the isopropylphenyl compounds were generally weaker than the corresponding t-butyl compounds. Methylation of the phenolic group led to loss of activity.

Study Snapshot

The dimethyl analogue of 3-(2,6-bis-iso-propyl-4-hydroxyphenyl)propan-1-ol shows the greatest activity as an allosteric modulator of GABAB receptors, with isopropylphenyl compounds generally weaker than t-but

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

Synthesis and biological activity of allosteric modulators of GABA B receptors part 3. 3-(2,6-bis-iso-propyl-4-hydroxyphenyl)propanols

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References

Gabaergic Synaptic Transmission: Molecular, Pharmacological, and Clinical Aspects

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Purification of Laboratory Chemicals

The Sixth Edition of "Purification of Laboratory Chemicals" provides updated coverage of the latest chemical products and processing techniques, safety, and hazards, while maintaining its focus on efficiency, results, and safety in chemical and biochemical laboratories.

Citations

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