Synthesis and inhibitory potential towards acetylcholinesterase, butyrylcholinesterase and lipoxygenase of some variably substituted chalcones.
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.
Hasan
Aurangzeb
A
Department of Chemistry, Quaid-i-Azam University, Islamabad-45320, Pakistan.
Khan
Khalid M
KM
Sher
Mohammed
M
Maharvi
Ghulam M
GM
Nawaz
Sarfraz A
SA
Choudhary
M I
MI
Atta-ur-Rahman
Supuran
Claudiu T
CT
D000110:Acetylcholinesterase / Q000737:chemistry* / Q000378:metabolism; D000818:Animals; D002091:Butyrylcholinesterase / Q000737:chemistry* / Q000378:metabolism; D047188:Chalcones / Q000138:chemical synthesis* / Q000494:pharmacology*; D002800:Cholinesterase Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D004593:Electrophorus / Q000378:metabolism; D006736:Horses; D020128:Inhibitory Concentration 50; D008084:Lipoxygenase / Q000737:chemistry* / Q000378:metabolism; D016859:Lipoxygenase Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D015394:Molecular Structure
D047188:Chalcones; D002800:Cholinesterase Inhibitors; D016859:Lipoxygenase Inhibitors; D008084:Lipoxygenase; D000110:Acetylcholinesterase; D002091:Butyrylcholinesterase