title: Synthesis and inhibitory potential towards acetylcholinesterase, butyrylcholinesterase and lipoxygenase of some variably substituted chalcones.
abstract: 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.
authors.affiliation: Department of Chemistry, Quaid-i-Azam University, Islamabad-45320, Pakistan.
authors.forename: Aurangzeb
authors.initials: A
authors.lastname: Hasan
authors.forename: Khalid M
authors.initials: KM
authors.lastname: Khan
authors.forename: Mohammed
authors.initials: M
authors.lastname: Sher
authors.forename: Ghulam M
authors.initials: GM
authors.lastname: Maharvi
authors.forename: Sarfraz A
authors.initials: SA
authors.lastname: Nawaz
authors.forename: M I
authors.initials: MI
authors.lastname: Choudhary
authors.lastname: Atta-ur-Rahman
authors.forename: Claudiu T
authors.initials: CT
authors.lastname: Supuran
mesh_terms: 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
chemical_list: D047188:Chalcones; D002800:Cholinesterase Inhibitors; D016859:Lipoxygenase Inhibitors; D008084:Lipoxygenase; D000110:Acetylcholinesterase; D002091:Butyrylcholinesterase