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Makale Tam Makale Uluslararası 2012

Synthesis and carbonic anhydrase inhibitory properties of novel bromophenols including natural products

Halis Turker BALAYDIN, Hakan SOYUT, Deniz Ekinci, Süleyman Göksu, Sukru Beydemir, Abdullah MENZEK, Ertan Şahin

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY Cilt 27 · Sayı 1 · ss. 43–50 · 01.02.2012
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Özet

(2-Bromo-3,4-dimethoxyphenyl) (3,4-dimethoxyphenyl) methanone (10) and its derivatives with Br, one dibromide and isomeric three tribromides, were synthesized. Demethylation of these compounds afforded a series of new bromophenols. Inhibition of human cytosolic carbonic anhydrase II (hCA II) isozyme by these new bromophenols and naturally occurring 3,4,6-tribromo-5-(2,5-dibromo-3,4-dihydroxybenzyl) benzene-1,2-diol (3), and 5,5'-methylenebis(3,4,6-tribromo-benzene-1,2-diol) (4) was investigated. The synthesized compounds showed carbonic anhydrase inhibitory capacities with IC50 values in the range of 0.7-372 mu M against hCA II. Some bromophenols investigated here showed effective hCA II inhibitory activity and might be used as leads for generating novel carbonic anhydrase inhibitors which are valuable drug candidates for the treatment of glaucoma, epilepsy, gastric and duodenal ulcers, neurological disorders, or osteoporosis.

Anahtar kelimeler

PATTERNS SERIES IN-VITRO carbonic anhydrase enzyme inhibition THERAPEUTIC APPLICATIONS phenols BROMOPHENOLS METALS diphenylmethane glaucoma

Atıf için künye

BALAYDIN, H. T., SOYUT, H., Ekinci, D., Göksu, S., Beydemir, S., MENZEK, A., & Şahin, E. (2012). Synthesis and carbonic anhydrase inhibitory properties of novel bromophenols including natural products. JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 27(1), 43–50. https://doi.org/10.3109/14756366.2011.574131

BibTeX
@article{balaydin2012-66717,
  author = {BALAYDIN, Halis Turker and SOYUT, Hakan and Ekinci, Deniz and Göksu, Süleyman and Beydemir, Sukru and MENZEK, Abdullah and Şahin, Ertan},
  title = {Synthesis and carbonic anhydrase inhibitory properties of novel bromophenols including natural products},
  journal = {JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY},
  year = {2012},
  volume = {27},
  number = {1},
  pages = {43--50},
  issn = {1475-6366},
  doi = {10.3109/14756366.2011.574131},
  url = {https://akademik.atauni.edu.tr/yayinlar/66717-synthesis-and-carbonic-anhydrase-inhibitory-properties-of-novel-bromophenols}
}