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Design, synthesis of novel peripherally tetra-chalcone substituted phthalocyanines and their inhibitory effects on acetylcholinesterase and carbonic anhydrases (hCA I and II)
Journal of Organometallic Chemistry ( IF 2.1 ) Pub Date : 2021-08-05 , DOI: 10.1016/j.jorganchem.2021.122021
Tayfun Arslan 1
Affiliation  

In this work, phthalocyanine precursor (3), tetra-chalcone substituted metal-free (4) and metallo phthalocyanines (5, 6, 7) were synthesized for the first time and surveyed interactions against acetylcholinesterase (AChE, which are associated with Alzheimer's disease) and human CA isoenzymes I and II (hCA I and hCA II, which are ubiquitous cytosolic isoforms). The structures of the novel phthalonitrile (3) and phthalocyanines (4-7) were designated by FT-IR, NMR, UV-Vis, and mass spectroscopy. These phthalocyanines inhibited hCA I with inhibition constants in the range of 0.5621-0.6413 μM and hCA II with inhibition constants in the range of 0.4823-0.6117 μM. On the other hand, these phthalocyanines indicated notable inhibitory effect against AChE.



中文翻译:

新型外周四查尔酮取代酞菁的设计、合成及其对乙酰胆碱酯酶和碳酸酐酶(hCA I 和 II)的抑制作用

在这项工作中,首次合成了酞菁前体 ( 3 )、四查耳酮取代的无金属 ( 4 ) 和金属酞菁 ( 5, 6, 7 ) 并调查了与乙酰胆碱酯酶 (AChE) 的相互作用,这些酶与阿尔茨海默病有关) 和人类 CA 同工酶 I 和 II(hCA I 和 hCA II,它们是普遍存在的胞质异构体)。新型邻苯二甲腈 ( 3 ) 和酞菁 ( 4 - 7 ) 的结构) 由 FT-IR、NMR、UV-Vis 和质谱法指定。这些酞菁以 0.5621-0.6413 μM 范围内的抑制常数抑制 hCA I,以 0.4823-0.6117 μM 范围内的抑制常数抑制 hCA II。另一方面,这些酞菁对 AChE 具有显着的抑制作用。

更新日期:2021-08-10
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