Novel multipotent phenylthiazole–tacrine hybrids for the inhibition of cholinesterase activity, β-amyloid aggregation and Ca 2+ overload

Y Wang, F Wang, JP Yu, FC Jiang, XL Guan…

Index: Wang, Yue; Wang, Fang; Guan, Xin-Lei; Wang, Can-Ming; Cao, Hui; Li, Ming-Xing; Chen, Jian-Guo; Jiang, Feng-Chao; Li, Lei; Yu, Jun-Ping Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 21 p. 6513 - 6522,10 Title/Abstract Full Text Show Details Wang, Yue; Wang, Fang; Yu, Jun-Ping; Jiang, Feng-Chao; Guan, Xin-Lei; Wang, Can-Ming; Li, Lei; Cao, Hui; Li, Ming-Xing; Chen, Jian-Guo Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 21 p. 6513 - 6522

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Citation Number: 16

Abstract

In this study, a series of multipotent phenylthiazole–tacrine hybrids (7a–7e, 8, and 9a–9m) were synthesized and biologically evaluated. Screening results showed that phenylthiazole– tacrine hybrids were potent cholinesterase inhibitors with pIC50 (− logIC50) value ranging from 5.78±0.05 to 7.14±0.01 for acetylcholinesterase (AChE), and from 5.75±0.03 to 10.35±0.15 for butyrylcholinesterase (BuChE). The second series of phenylthiazole– ...