Synthesis and paroxonase activities of novel bromophenols

被引：54

作者：

Akbaba, Yusuf ^{[1
]}

Turkes, Cuneyt ^{[1
]}

Polat, Leyla ^{[1
]}

Soyut, Hakan ^{[1
]}

Sahin, Ertan ^{[1
]}

Menzek, Abdullah ^{[1
]}

Goksu, Suleyman ^{[1
]}

Beydemir, Sukru ^{[1
]}

机构：

[1] Ataturk Univ, Dept Chem, Fac Sci, TR-25240 Erzurum, Turkey

来源：

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY | 2013年 / 28卷 / 05期

关键词：

Bromination; bromophenols; natural products; demethylation; paroxonase activity; IN-VITRO; CARBONIC-ANHYDRASE; PARAOXONASE; ANESTHETICS; PON1;

D O I：

10.3109/14756366.2012.715287

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

070307 [化学生物学]; 071010 [生物化学与分子生物学];

摘要：

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] .

引用

页码：1073 / 1079

页数：7

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