Ağrı İbrahim Çeçen University, Science and Art Faculty, Chemistry Department, Ağrı, Turkey.
J Enzyme Inhib Med Chem. 2012 Jun;27(3):365-9. doi: 10.3109/14756366.2011.591290. Epub 2011 Jun 23.
Studies on carbonic anhydrase (CA, EC 4.2.1.1) inhibitors have increased due to several therapeutic applications while there are few investigations on activators. Here we investigated CA inhibitory and activatory capacities of a series of dopaminergic compounds on human carbonic anhydrase (hCA) isozymes I, II, and VI. 2-Amino-1,2,3,4-tetrahydronaphthalene-6,7-diol hydrobromide and 2-amino-1,2,3,4-tetrahydronaphthalene-5,6-diol hydrobromide were found to show effective inhibitory action on hCA I and II whereas 2-amino-5,6-dibromoindan hydrobromide and 2-amino-5-bromoindan hydrobromide exhibited only moderate inhibition against both isoforms, being more effective inhibitors of hCA VI. K(i) values of the molecules 3-6 were in the range of 41.12-363 μM against hCA I, of 0.381-470 μM against hCA II and of 0.578-1.152 μM against hCA VI, respectively. Compound 7 behaved as a CA activator with K(A) values of 27.3 μM against hCA I, of 18.4 μM against hCA II and of 8.73 μM against hCA VI, respectively.
由于多种治疗应用，碳酸酐酶 (CA，EC 4.2.1.1) 抑制剂的研究有所增加，而对其激活剂的研究却很少。在这里，我们研究了一系列多巴胺化合物对人碳酸酐酶 (hCA) 同工酶 I、II 和 VI 的抑制和激活作用。发现 2-氨基-1,2,3,4-四氢萘-6,7-二醇氢溴酸盐和 2-氨基-1,2,3,4-四氢萘-5,6-二醇氢溴酸盐对 hCA I 和 II 表现出有效的抑制作用，而 2-氨基-5,6-二溴茚满氢溴酸盐和 2-氨基-5-溴茚满氢溴酸盐对两种同工酶仅表现出中等抑制作用，对 hCA VI 的抑制作用更强。分子 3-6 的 K(i) 值范围分别为 41.12-363 μM 对 hCA I，0.381-470 μM 对 hCA II 和 0.578-1.152 μM 对 hCA VI。化合物 7 表现为 CA 激活剂，对 hCA I 的 K(A) 值为 27.3 μM，对 hCA II 的 K(A) 值为 18.4 μM，对 hCA VI 的 K(A) 值为 8.73 μM。
