Hasan Aurangzeb, Khan Khalid M, Sher Mohammed, Maharvi Ghulam M, Nawaz Sarfraz A, Choudhary M I, Supuran Claudiu T
Department of Chemistry, Quaid-i-Azam University, Islamabad-45320, Pakistan.
J Enzyme Inhib Med Chem. 2005 Feb;20(1):41-7. doi: 10.1080/14756360400015231.
A series of variably substituted chalcones were synthesized by condensation of substituted acetophenones with mono-, di- or trisubstituded benzaldehydes. It was observed that some of these compounds have the potential to inhibit acetylcholinesterase, whereas others show activity against butyrylcholinesterase, depending on the substitution pattern at the two aromatic rings of these chalcones. Similarly, lipoxygenase was inhibited by two of these compounds. It has been observed that inhibition of the three enzymes was concentration dependent with the IC50 values ranging from 28.2-134.5 microM against acetylcholinesterase, 16.0-23.1 microM against butyrylcholinesterase and 57.6-71.7 microM against lipoxygenase, respectively.
通过取代苯乙酮与单取代、二取代或三取代苯甲醛缩合，合成了一系列可变取代的查耳酮。据观察，这些化合物中的一些有抑制乙酰胆碱酯酶的潜力，而其他化合物则根据这些查耳酮两个芳香环上的取代模式显示出对丁酰胆碱酯酶的活性。同样，其中两种化合物抑制了脂氧合酶。据观察，对这三种酶的抑制作用呈浓度依赖性，对乙酰胆碱酯酶的IC50值范围为28.2 - 134.5微摩尔，对丁酰胆碱酯酶为16.0 - 23.1微摩尔，对脂氧合酶为57.6 - 71.7微摩尔。
