title: [Design, synthesis and evaluation of new L-proline derivatives as acetylcholinesterase inhibitors].
abstract: In this paper, fourteen new L-proline derivatives were designed and synthesized, and their acetlcholinesterase (AChE) inhibitory activities were also investigated in vitro. New L-proline derivatives were prepared from substituted 2-bromo-1-acetophenones through four-step reaction; and their bioactivities as AChE inhibitors were measured by Ellman spectrophotometry. The results showed that the target compounds had a certain AChE inhibitory activity to in vitro. The bioactivity of compound 8b was the best of them, and its IC50 value was 5.45 µmol.L-1, which was better than that of rivastigmine. So the acetylcholinesterase inhibitory activities of new L-proline derivatives were worth to be further studied.
authors.forename: Yun-feng
authors.initials: YF
authors.lastname: Tian
authors.forename: Jun-tao
authors.initials: JT
authors.lastname: Chen
authors.forename: Jun-jie
authors.initials: JJ
authors.lastname: Li
authors.forename: Ying-chao
authors.initials: YC
authors.lastname: Zhang
authors.forename: Ting-ting
authors.initials: TT
authors.lastname: Cao
authors.forename: Zheng-yue
authors.initials: ZY
authors.lastname: Ma
mesh_terms: D000110:Acetylcholinesterase; D002800:Cholinesterase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry; D015195:Drug Design; D011392:Proline / Q000031:analogs & derivatives*; D000068836:Rivastigmine / Q000737:chemistry; D013329:Structure-Activity Relationship
chemical_list: D002800:Cholinesterase Inhibitors; D011392:Proline; D000110:Acetylcholinesterase; D000068836:Rivastigmine