Acetylcholinesterase and Butyrylcholinesterase Inhibitory Activities of 5-Arylidene-N, N-Diethylthiobarbiturates

摘要

5-Arylidene-N,N-diethylthiobarbiturates 1-25 were evaluated for their potential against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes and displayed varying degree of inhibition. Based on the IC50 values, compound 6 (IC50 = 92.51 +/- 0.01 mu M) was the only active compound against acetylcholinesterase, however this compound was also weakly active against butyrylcholinesterase with an IC50 value 124.76 +/- 0.02 mu M. Six compounds 1, 6, 7, 16, 17, and 18 showed weak inhibition against BChE, among them compound 18 (IC50 = 82.25 +/- 0.07 mu M) showed good inhibition against BChE. Nevertheless, compounds 1, 7, 16, 17, and 18 were selectively active against BChE enzyme.