Synthesis and biological evaluation of some 1‐naphthol derivatives as antioxidants, acetylcholinesterase, and carbonic anhydrase inhibitors
作者:Musa Erdoğan、Leyla Polat Köse、Selçuk Eşsiz、İlhami Gülçin
DOI:10.1002/ardp.202100113
日期:——
A series of some naphthol derivatives 4a–f, 5a,f, 6a, and 7a,b (six novel ones: 4c,d, 5a, 6a, 7a,b) bearing F, Cl, Br, OMe, and dioxole substituents at different positions of the aromatic rings was designed, synthesized, and characterized. The naphthol derivatives were synthesized in three steps, namely the addition reaction of furan via Diels–Alder cycloaddition reaction, copper(II) trifluoromethanesulfonate
一系列一些萘酚衍生物4a – f , 5a , f , 6a , 和7a , b (六个新的: 4c,d , 5a , 6a , 7a,b ) 带有 F, Cl, Br, OMe, and dioxole 取代基在设计、合成和表征了芳环的不同位置。萘酚衍生物的合成分三步进行,即通过 Diels-Alder 环加成反应与呋喃的加成反应、三氟甲磺酸铜 (II) (Cu(OTf) 2)-催化的芳构化反应和溴化反应。新获得的化合物(4c、d、5a、6a、7a、b)的结构通过光谱技术表征。此外,在体外条件下研究了一些生物活性研究。对从人类红细胞中纯化的人类碳酸酐酶 (hCA) I 和 II 同工酶进行了这些化合物的抑制研究,作为生物学评价。此外,它们的潜在抗氧化和抗自由基活性通过 ABTS •+等分析方法进行了研究。和 DPPH• 清除,并确定一些分子表现出良好的活性。此外,还测试了乙酰胆碱酯酶 (