期刊
MOLECULES
卷 27, 期 21, 页码 -出版社
MDPI
DOI: 10.3390/molecules27217426
关键词
bromophenol; diaryl methane; demethylation; carbonic anhydrase; acetylcholinesterase
资金
- Ataturk University Erzurum [FBA-2017-6124]
Nine new bromophenol derivatives were designed and synthesized in this study, showing effective inhibition effects on metabolic enzymes. These compounds may be used for the treatment of various diseases.
In this work, nine new bromophenol derivatives were designed and synthesized. The alkylation reactions of (2-bromo-4,5-dimethoxyphenyl)methanol (7) with substituted benzenes 8-12 produced new diaryl methanes 13-17. Targeted bromophenol derivatives 18-21 were synthesized via the O-Me demethylation of diaryl methanes with BBr3. Moreover, the synthesized bromophenol compounds were tested with some metabolic enzymes such as acetylcholinesterase (AChE), carbonic anhydrase I (CA I), and II (CA II) isoenzymes. The novel synthesized bromophenol compounds showed Ki values that ranged from 2.53 +/- 0.25 to 25.67 +/- 4.58 nM against hCA I, from 1.63 +/- 0.11 to 15.05 +/- 1.07 nM against hCA II, and from 6.54 +/- 1.03 to 24.86 +/- 5.30 nM against AChE. The studied compounds in this work exhibited effective hCA isoenzyme and AChE enzyme inhibition effects. The results show that they can be used for the treatment of glaucoma, epilepsy, Parkinson's as well as Alzheimer's disease (AD) after some imperative pharmacological studies that would reveal their drug potential.
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