Synthesis and paroxonase activities of novel bromophenols

doi:10.3109/14756366.2012.715287

Paper

Synthesis and paroxonase activities of novel bromophenols

Published Sep 10, 2013 · Yusuf Akbaba, Cüneyt Türkeş, Leyla Polat

Journal of Enzyme Inhibition and Medicinal Chemistry

53

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1

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Abstract

Three novel bromophenols 10–12 were synthesized. Acylation of veratrole (4) with 2,3-dimethoxy benzoic acid (5) gave a kown diarylmethanone 6. Bromination of 6 with different equivalents of molecular bromine afforded new di and tribrominated compounds 7–9 which were converted to their corresponding bromophenols 10–12 via O-demethylation with BBr3. Paraoxonase-1 (PON1) was purified from human serum with approximately 42% and 3584 U × mg−1 specific activity. The synthesized compounds 6–12 showed inhibitory effects on paraoxonase-1 (PON1) which is an organophosphate (OP) hydrolyser and an antioxidant bioscavenger enzyme. IC50 values were determined in the range of 0.123–1.212 mM. Graphical abstract

In Vitro Study

Study Snapshot

Novel bromophenols 10-12 show inhibitory effects on paraoxonase-1, an organophosphate hydrolyser and antioxidant bioscavenger enzyme, with IC50 values ranging from 0.123 to 1.12 mM.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

Synthesis and paroxonase activities of novel bromophenols

References

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