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J Enzyme Inhib Med Chem. 2013 Oct;28(5):1073-9. doi: 10.3109/14756366.2012.715287. Epub 2012 Sep 20.

Synthesis and paroxonase activities of novel bromophenols.

Author information

1
Department of Chemistry, Faculty of Science, Atatürk University , Erzurum , Turkey.

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.

PMID:
22994801
DOI:
10.3109/14756366.2012.715287
[Indexed for MEDLINE]

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