Atatürk University, Faculty of Science, Department of Chemistry, 25240 Erzurum, Turkey.
Eur J Med Chem. 2012 Aug;54:423-8. doi: 10.1016/j.ejmech.2012.05.025. Epub 2012 May 27.
A series of bisphenol, bromophenol, and methoxyphenol derivatives (2-24) including the natural bromophenols vidalol B, 3,4,6-tribromo-5-(2,5-dibromo-3,4-dihydroxybenzyl)benzene-1,2-diol (2) and 5,5'-methylenebis(3,4,6-tribromo-benzene-1,2-diol) (3) were prepared. In the current study, inhibition of four human carbonic anhydrase (hCA, EC 4.2.1.1) isozymes, I, II, IV, and VI, with these compounds 2-24 was investigated. The compounds 2-24 were found to be promising carbonic anhydrase inhibitors, some of which showed interesting inhibitory activities. 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.
一系列的双酚、溴酚和甲氧基酚衍生物（2-24），包括天然溴酚 vidalol B、3,4,6-三溴-5-(2,5-二溴-3,4-二羟基苄基)苯-1,2-二醇（2）和 5,5'-亚甲基双(3,4,6-三溴苯-1,2-二醇)（3），被制备出来。在本研究中，抑制了四种人碳酸酐酶（hCA，EC 4.2.1.1）同工酶，I、II、IV 和 VI，用这些化合物 2-24 进行了研究。发现这些化合物 2-24 是很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。本文研究的一些化合物表现出有效的 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、胃溃疡和十二指肠溃疡、神经紊乱和骨质疏松症等疾病的有价值的药物候选物。
