标题：Design, synthesis and biological evaluation of tacrine-1,2,3-triazole derivatives as potent cholinesterase inhibitors
作者：Wu, Gaochan; Gao, Yun; Kang, Dongwei; Huang, Boshi; Huo, Zhipeng; Liu, Huiqing; Poongavanam, Vasanthanathan; Zhan, Peng; Liu, Xinyong
作者机构：[Wu, Gaochan; Gao, Yun; Kang, Dongwei; Huang, Boshi; Huo, Zhipeng; Zhan, Peng; Liu, Xinyong] Shandong Univ, Sch Pharmaceut Sci, Minist Educ, Dept Med 更多
通讯作者：Zhan, P;Liu, XY;Poongavanam, V
通讯作者地址：[Zhan, P; Liu, XY]Shandong Univ, Sch Pharmaceut Sci, Minist Educ, Dept Med Chem,Key Lab Chem Biol, 44 West Culture Rd, Jinan 250012, Shandong, Peoples 更多
摘要：We report herein the design and synthesis of a series of 11 novel tacrine-1,2,3-triazole derivatives via a Cu(I)-catalyzed alkyne-azide 1,3-dipolar cycloaddition (CuAAC) reaction. The newly synthesized compounds were evaluated for their inhibition activity against Electrophorus electricus acetylcholinesterase (AChE) and horse serum butyrylcholinesterase (BChE) as potential drug targets for Alzheimer's disease (AD). Among the designed compounds, compound 8a2 exhibited potent inhibition against AChE and BChE with IC50 values of 4.89 mu M and 3.61 mu M, respectively. Further structure-activity relationship (SAR) and molecular modeling studies may provide valuable insights into the design of better tacrine-triazole analogues with potential therapeutic applications for AD.