Section of Pharmaceutical and Nutraceutical Sciences, Department of Neuroscience, Psychology, Drug Research and Child's Health, University of Florence, Sesto Fiorentino, Italy.
J Enzyme Inhib Med Chem. 2020 Dec;35(1):1003-1010. doi: 10.1080/14756366.2020.1749602.
The Carbonic Anhydrase (CA, EC 4.2.1.1) activating properties of histamine have been known for a long time. This compound has been extensively modified but only in few instances the imidazole ring has been replaced with other heterocycles. It was envisaged that the imidazoline ring could be a bioisoster of the imidazole moiety. Indeed, we report that clonidine, a 2-aminoimidazoline derivative, was found able to activate several human CA isoforms (hCA I, IV, VA, VII, IX, XII and XIII), with potency in the micromolar range, while it was inactive on hCA II. A series of 2-aminoimidazoline, structurally related to clonidine, was then synthesised and tested on selected hCA isoforms. The compounds were inactive on hCA II while displayed activating properties on hCA I, VA, VII and XIII, with K values in the micromolar range. Two compounds ( and ) showed some preference for the hCA VA or VII isoforms.
组胺的碳酸酐酶（CA，EC 4.2.1.1）激活特性早已为人所知。这种化合物已经被广泛修饰，但只有在少数情况下，咪唑环被其他杂环所取代。人们设想咪唑啉环可以作为咪唑部分的生物等排体。事实上，我们报告说，可乐定，一种 2-氨基咪唑啉衍生物，被发现能够激活几种人碳酸酐酶同工酶（hCA I、IV、VA、VII、IX、XII 和 XIII），其活性在微摩尔范围内，而对 hCA II 则没有活性。然后合成了一系列与可乐定结构相关的 2-氨基咪唑啉，并在选定的 hCA 同工酶上进行了测试。这些化合物对 hCA II 没有活性，而对 hCA I、VA、VII 和 XIII 具有激活作用，其 K 值在微摩尔范围内。两种化合物（和）对 hCA VA 或 VII 同工酶表现出一定的选择性。
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