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

Date

2012

Author

Balaydin, Halis Turker
Soyut, Hakan
Ekinci, Deniz
Goksu, Suleyman
Beydemir, Sukru
Menzek, Abdullah
Sahin, Ertan

Metadata

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Abstract

(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.

Source

Journal of Enzyme Inhibition and Medicinal Chemistry

Volume

27

Issue

1

URI

https://doi.org/10.3109/14756366.2011.574131
https://hdl.handle.net/20.500.12712/16683

Collections

  • PubMed İndeksli Yayınlar Koleksiyonu [6144]
  • Scopus İndeksli Yayınlar Koleksiyonu [14046]
  • WoS İndeksli Yayınlar Koleksiyonu [12971]



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