新型环己酮基溴苯酚衍生物的合成及碳酸酐酶抑制活性。
Synthesis and carbonic anhydrase inhibitory properties of novel cyclohexanonyl bromophenol derivatives.
机构信息
Artvin Çoruh University, Education Faculty, 08000 Artvin, Turkey.
出版信息
Bioorg Med Chem Lett. 2012 Feb 1;22(3):1352-7. doi: 10.1016/j.bmcl.2011.12.069. Epub 2011 Dec 21.
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.
天然存在的新型环己酮基溴苯酚 2(R)-2-(2,3,6-三溴-4,5-二羟基苄基)环己酮（4）被合成成为外消旋化合物。还获得了带有 Br、OMe、CO 和 OH 的环己基苯基甲烷衍生物（10-17）。用化合物 2-4、8 和 10-26 研究了对四种人碳酸酐酶（hCA，EC 4.2.1.1）同工酶 I、II、IV 和 VI 的抑制作用。这些化合物被发现是有前途的碳酸酐酶抑制剂，其中一些表现出有趣的抑制活性。这里研究的一些化合物显示出有效的 hCA 抑制活性，并且可能被用作生成新型碳酸酐酶抑制剂的先导化合物，这些抑制剂是治疗青光眼、癫痫、胃和十二指肠溃疡、神经紊乱和骨质疏松症的有价值的药物候选物。
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