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Makale Tam Makale Uluslararası 2013

Synthesis and paroxonase activities of novel bromophenols

Yusuf AKBABA, Cuneyt TURKES, Leyla POLAT, Hakan SOYUT, Ertan Şahin, Abdullah MENZEK, Süleyman Göksu, Sukru Beydemir

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY Cilt 28 · Sayı 5 · ss. 1073–1079 · 01.10.2013
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Özet

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.

Anahtar kelimeler

IN-VITRO carbonic anhydrase Natural products BROMOPHENOLS PON1 Bromination demethylation paroxonase activity PARAOXONASE ANESTHETICS

Atıf için künye

AKBABA, Y., TURKES, C., POLAT, L., SOYUT, H., Şahin, E., MENZEK, A., Göksu, S., & Beydemir, S. (2013). Synthesis and paroxonase activities of novel bromophenols. JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 28(5), 1073–1079. https://doi.org/10.3109/14756366.2012.715287

BibTeX
@article{akbaba2013-66661,
  author = {AKBABA, Yusuf and TURKES, Cuneyt and POLAT, Leyla and SOYUT, Hakan and Şahin, Ertan and MENZEK, Abdullah and Göksu, Süleyman and Beydemir, Sukru},
  title = {Synthesis and paroxonase activities of novel bromophenols},
  journal = {JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY},
  year = {2013},
  volume = {28},
  number = {5},
  pages = {1073--1079},
  issn = {1475-6366},
  doi = {10.3109/14756366.2012.715287},
  url = {https://akademik.atauni.edu.tr/yayinlar/66661-synthesis-and-paroxonase-activities-of-novel-bromophenols}
}