期刊
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
卷 28, 期 5, 页码 1073-1079出版社
TAYLOR & FRANCIS LTD
DOI: 10.3109/14756366.2012.715287
关键词
Bromination; bromophenols; natural products; demethylation; paroxonase activity
资金
- TUBITAK (The Scientific and Technological Research Council of Turkey) [TBAG-107T348]
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 x 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. [GRAPHICS] .
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