三唑取代的无金属、金属酞菁及其水溶性衍生物作为潜在的胆碱酯酶抑制剂：设计、合成及体外抑制研究。
Triazole substituted metal-free, metallo-phthalocyanines and their water soluble derivatives as potential cholinesterases inhibitors: Design, synthesis and in vitro inhibition study.
机构信息
Giresun University, Faculty of Science, Department of Chemistry, 28200 Giresun, Turkey; Giresun University, Technical Sciences Vocational School, Department of Textile, Giresun University, 28049 Giresun, Turkey.
Giresun University, Faculty of Science, Department of Chemistry, 28200 Giresun, Turkey.
出版信息
Bioorg Chem. 2019 Sep;90:103100. doi: 10.1016/j.bioorg.2019.103100. Epub 2019 Jul 3.
In this study, 1,2,3-triazole substituted metal-free and metallo phthalocyanines (4, 5, 6) and their water soluble derivatives (4a, 5a, 6a) were designed, synthesized for the first time and tested in vitro on acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes. Most phthalocyanines exhibited good inhibitory activities on these enzymes. Among the six phthalocyanines and starting compounds, 4a showed the most interesting profile as a submicromolar selective inhibitor of AChE (IC = 0.040 µM) and 5a showed the most effective inhibitor of BChE (IC = 0.1198 µM).
在这项研究中，首次设计、合成了 1,2,3-三唑取代的无金属和金属酞菁（4、5、6）及其水溶性衍生物（4a、5a、6a），并在体外对乙酰胆碱酯酶（AChE）和丁酰胆碱酯酶（BChE）进行了测试。大多数酞菁对这些酶表现出良好的抑制活性。在这六种酞菁和起始化合物中，4a 作为 AChE 的亚微摩尔选择性抑制剂（IC = 0.040 µM）表现出最有趣的特性，而 5a 作为 BChE 的最有效抑制剂（IC = 0.1198 µM）。
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