Bioorganic & medicinal chemistry

Synthesis and biological evaluation of berberine–thiophenyl hybrids as multi-functional agents: Inhibition of acetylcholinesterase, butyrylcholinesterase, and Aβ …

T Su, S Xie, H Wei, J Yan, L Huang, X Li

Index: Su, Tao; Xie, Shishun; Wei, Hui; Yan, Jun; Huang, Ling; Li, Xingshu Bioorganic and Medicinal Chemistry, 2013 , vol. 21, # 18 p. 5830 - 5840

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Citation Number: 12

Abstract

Abstract A series of berberine–thiophenyl hybrids were designed, synthesised, and evaluated as inhibitors of acetylcholinesterase (AChE), butyrylcholinesterase (BuChE) and β- amyloid (Aβ) aggregation and as antioxidants. Among these hybrids, compounds 4f and 4i, berberine linked with o-methylthiophenyl and o-chlorothiophenyl by a 2-carbon spacer, were observed to be potent inhibitors of AChE, with IC 50 values of 0.077 and 0.042 μM, ...