Medical Laboratory Techniques Program, Vocational School of Health Services, Batman University, Batman, Turkey.
Department of Chemistry and Chemical Processing Technologies, Vocational School of Technical Sciences, Batman University, Batman, Turkey.
Arch Pharm (Weinheim). 2022 Apr;355(4):e2100430. doi: 10.1002/ardp.202100430. Epub 2022 Jan 7.
In this study, a series of novel Schiff base derivatives containing a pyrazolone ring (2a-e) were designed, successfully synthesized for the first time, and characterized by elemental analysis and some spectroscopic methods. These compounds were tested for their inhibitory activities on acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and the human carbonic anhydrase isoenzymes I and II (hCA I and II). All synthesized molecules indicated significant inhibition effects with IC values ranging from 14.15 to 107.62 nM against these enzymes. Compound 2d showed the most potent inhibitory activity among the tested molecules toward AChE and BChE (IC = 15.07 and 14.15 nM) compared to the standard drug neostigmine. We determined that the IC values of the tested molecules ranged between 16.86 and 57.96 nM for hCA I and 15.24-46.21 nM for hCA II. As a consequence, we may say that some of the Schiff base derivatives may be used as potential drug candidates in later studies.
在这项研究中，设计了一系列含有吡唑啉酮环的新型席夫碱衍生物（2a-e），首次成功合成，并通过元素分析和一些光谱方法进行了表征。这些化合物被测试了它们对乙酰胆碱酯酶（AChE）、丁酰胆碱酯酶（BChE）以及人碳酸酐酶同工酶 I 和 II（hCA I 和 II）的抑制活性。所有合成的分子都表现出显著的抑制作用，IC 值范围为 14.15 到 107.62 nM。与标准药物新斯的明相比，化合物 2d 对 AChE 和 BChE 的抑制活性最强（IC 分别为 15.07 和 14.15 nM）。我们确定，测试分子对 hCA I 的 IC 值范围在 16.86 到 57.96 nM 之间，对 hCA II 的 IC 值范围在 15.24 到 46.21 nM 之间。因此，我们可以说，一些席夫碱衍生物可能在以后的研究中被用作潜在的药物候选物。
