New anthrarobin acyl derivatives as butyrylcholinesterase inhibitors: synthesis, in vitro and in silico studies.

ABSTRACT: To treat Alzheimer's disease (AD), the available candidates are effective only against mild AD or have side effects. So, a study was planned to synthesis new candidates that may have good potential to treat AD. A series of new anthrarobin acyl derivatives (2-8) were synthesized by the reaction of anthrarobin (1) and acetic anhydride/acyl chlorides. The product were characterized by ¹H NMR and EI-MS, and evaluated for butyrylcholinesterase (BuChE) inhibition activity. Compounds 5 and 4 showed notable BuChE inhibitory potential with IC₅₀ 5.3 ± 1.23 and 17.2 ± 0.47 μM, respectively when compared with the standard eserine (IC₅₀ 7.8 ± 0.27 μM), compound 5 showed potent BuChE inhibition potential than the standard eserine

SUBMITTER: Lateef M 

PROVIDER: S-EPMC5506883 | biostudies-literature | 2017 Jul

REPOSITORIES: biostudies-literature