Bayrak_2018_Bioorg.Chem_85_128

Reference

Title : The first synthesis, carbonic anhydrase inhibition and anticholinergic activities of some bromophenol derivatives with S including natural products - Bayrak_2018_Bioorg.Chem_85_128
Author(s) : Bayrak C , Taslimi P , Karaman HS , Gulcin I , Menzek A
Ref : Bioorg Chem , 85 :128 , 2018
Abstract :

Starting from vanillin, known four benzyl bromides with Br were synthesized. The first synthesis of natural product 3,4-dibromo-5-((methylsulfonyl)methyl)benzene-1,2-diol (2) and 3,4,6-tribromo-5-((methylsulfonyl)methyl)benzene-1,2-diol (3) and derivatives were carried out by demethylation, acetylatilation, oxidation and hydrolysis reactions of the benzyl bromides. Also, these compounds were tested against some important enzymes like acetylcholinesterase and butyrylcholinesterase enzymes, carbonic anhydrase I, and II isoenzymes. The novel bromophenols showed Ki values of in range of 53.75+/-12.54-234.68+/-46.76nM against hCA I, 42.84+/-9.36 and 200.54+/-57.25nM against hCA II, 0.84+/-0.12-14.63+/-3.06nM against AChE and 0.93+/-0.20-18.53+/-5.06nM against BChE. Induced fit docking process performed on the compounds inhibiting hCA I, hCA II, AChE, and BChE receptors. Hydroxyl group should exist at the aromatic ring of the compounds for inhibition of the enzymes. The moieties reported in this study will be useful for design of more potent and selective inhibitors against the enzymes.

PubMedSearch : Bayrak_2018_Bioorg.Chem_85_128
PubMedID: 30605886

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Citations formats

Bayrak C, Taslimi P, Karaman HS, Gulcin I, Menzek A (2018)
The first synthesis, carbonic anhydrase inhibition and anticholinergic activities of some bromophenol derivatives with S including natural products
Bioorg Chem 85 :128

Bayrak C, Taslimi P, Karaman HS, Gulcin I, Menzek A (2018)
Bioorg Chem 85 :128