Synthesis and paroxonase activities of novel bromophenols
Open Access
- 20 September 2012
- journal article
- Published by Taylor & Francis Ltd in Journal of Enzyme Inhibition and Medicinal Chemistry
- Vol. 28 (5), 1073-1079
- https://doi.org/10.3109/14756366.2012.715287
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 abstractKeywords
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