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Synthesis and carbonic anhydrase inhibitory properties of novel cyclohexanonyl bromophenol derivatives.

Abstract：

:The Naturally occurring novel cyclohexanonyl bromophenol 2(R)-2-(2,3,6-tribromo-4,5-dihydroxybenzyl)cyclohexanone (4) was synthesized as a racemic compound. Cyclohexylphenyl methane derivatives (10-17) with Br, OMe, CO, and OH were also obtained. Inhibition of four human carbonic anhydrase (hCA, EC 4.2.1.1) isozymes I, II, IV, and VI, with compounds 2-4, 8, and 10-26 was investigated. These compounds were found to be promising carbonic anhydrase inhibitors and some of them showed interesting inhibitory activity. Some of the compounds investigated here showed effective hCA 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, and osteoporosis.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Balaydın HT,Sentürk M,Menzek A

doi

10.1016/j.bmcl.2011.12.069

subject

Has Abstract

pub_date

2012-02-01 00:00:00

pages

1352-7

issue

3

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(11)01750-1

journal_volume

22

pub_type

杂志文章

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