Synthesis and inhibitory potential towards acetylcholinesterase, butyrylcholinesterase and lipoxygenase of some variably substituted chalcones

被引:44
作者
Hasan, A
Khan, KM
Sher, M
Maharvi, GM
Nawaz, SA
Choudhary, MI
Atta-ur-Rahman
Supuran, CT
机构
[1] Univ Florence, Dipartimento Chim, Lab Chim Bioinorgan, I-50019 Florence, Italy
[2] Quaid i Azam Univ, Dept Chem, Islamabad 45320, Pakistan
[3] Univ Karachi, Int Ctr Chem Sci, HEJ Res Inst Chem, Karachi 75270, Pakistan
关键词
chalcones; acetylcholinesterase; butyrylcholinesterase; lipoxygenase;
D O I
10.1080/14756360400015231
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
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 muM against acetylcholinesterase, 16.0-23.1 muM against butyrylcholinesterase and 57.6-71.7 muM against lipoxygenase, respectively.
引用
收藏
页码:41 / 47
页数:7
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