新型 N-丙基邻苯二甲酰亚胺和 4-乙烯基苄基取代苯并咪唑盐的合成、表征及其对乙酰胆碱酯酶和碳酸酐酶金属螯合作用和抑制谱的测定。
Novel N-propylphthalimide- and 4-vinylbenzyl-substituted benzimidazole salts: Synthesis, characterization, and determination of their metal chelating effects and inhibition profiles against acetylcholinesterase and carbonic anhydrase enzymes.
机构信息
Department of Chemistry, Faculty of Arts and Sciences, Inönü University, Malatya 44280, Turkey.
Department of Chemistry, Faculty of Sciences, Atatürk University, Erzurum 25240, Turkey.
出版信息
J Biochem Mol Toxicol. 2018 Jan;32(1). doi: 10.1002/jbt.22009. Epub 2017 Nov 17.
The novel N-propylphthalimide-substituted and 4-vinylbenzyl-substituted N-heterocyclic carbene (NHC) precursors were synthesized by N-substituted benzimidazolium with aryl halides. The novel N-propylphthalimide-substituted and 4-vinylbenzyl-substituted NHC precursors have been characterized by using H NMR, C NMR, FTIR spectroscopy, and elemental analysis techniques. They were tested for the inhibition of AChE and hCA enzymes and demonstrated efficient inhibition profiles with K values in the range of 351.0-1269.9 nM against hCA I, 346.6-1193.1 nM against hCA II, and 19.0-76.3 nM against AChE. On the other hand, acetazolamide, a clinically used molecule, utilized as CA inhibitor, obtained a K value of 1246.7 nM against hCA I and 1407.6 nM against hCA II. Additionally, tacrine inhibited AChE and obtained a K value of 174.6 nM.
新型 N-丙基邻苯二甲酰亚胺取代和 4-乙烯基苄基取代 N-杂环卡宾（NHC）前体通过 N-取代苯并咪唑与芳基卤化物合成。新型 N-丙基邻苯二甲酰亚胺取代和 4-乙烯基苄基取代 NHC 前体通过 1 H NMR、13 C NMR、FTIR 光谱和元素分析技术进行了表征。它们被测试用于抑制 AChE 和 hCA 酶，并表现出有效的抑制谱，K 值范围为 351.0-1269.9 nM 对抗 hCA I，346.6-1193.1 nM 对抗 hCA II，19.0-76.3 nM 对抗 AChE。另一方面，乙酰唑胺是一种临床使用的分子，用作 CA 抑制剂，对 hCA I 的 K 值为 1246.7 nM，对 hCA II 的 K 值为 1407.6 nM。此外，他克林抑制 AChE，K 值为 174.6 nM。
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