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首页> 外文期刊>Journal of enzyme inhibition and medicinal chemistry. >Synthesis and characterization of complexes of a novel proton transfer salt and their inhibition studies on carbonic anhydrase isoenzymes
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Synthesis and characterization of complexes of a novel proton transfer salt and their inhibition studies on carbonic anhydrase isoenzymes

机译：新型质子转移盐配合物的合成，表征及其对碳酸酐酶同工酶的抑制作用

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A novel proton transfer compound (HClABT)+(HDPC.H2DPC)? (1) and its Fe(III), Co(II), Ni(II) and two different Cu(II) complexes (2–6) have been prepared and characterized by spectroscopic techniques. Additionally, single crystal X-ray diffraction techniques were applied to all complexes. All compounds, including acetazolamide (AAZ) as the control compound, were also evaluated for their in vitro inhibition effects on human hCA I and hCA II for their hydratase and esterase activities. Although there is no inhibition for hydratase activities, all compounds have inhibited the esterase activities of hCA I and II. The comparison of the inhibition studies of 1–6 to parent compounds, ClABT and H2DPC, indicates that 1–6 have superior inhibitory effects. The inhibition effects of 2–6 are also compared to the inhibitory properties of the simple metal complexes of ClABT and H2DPC, revealing an improved transfection profile. Data have been analysed by using a one-way analysis of variance for multiple comparisons.
机译：新型质子转移化合物（HClABT） + （HDPC.H 2 DPC）？（1）及其Fe（III），Co（ II），Ni（II）和两种不同的Cu（II）配合物（2-6）已经制备并通过光谱技术表征。此外，将单晶X射线衍射技术应用于所有配合物。还评估了所有化合物，包括乙酰唑酰胺（AAZ）作为对照化合物，它们在体外对人hCA I和hCA II的水合酶和酯酶活性具有抑制作用。尽管对水合酶活性没有抑制作用，但所有化合物均抑制了hCA I和II的酯酶活性。比较了1-6对母体化合物ClABT和H 2 DPC的抑制作用，结果表明1-6具有更好的抑制作用。还比较了2–6的抑制作用与ClABT和H 2 DPC的简单金属络合物的抑制性质，揭示了改善的转染特性。通过使用单向方差分析进行多次比较来分析数据。

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