Synthesis and in vitro evaluation of novel N-cycloalkylcarbamates as potential cholinesterase inhibitors

被引:4
作者
Horakova, Eva [1 ]
Drabina, Pavel [1 ]
Bruckova, Lenka [2 ]
Stepankova, Sarka [2 ]
Vorcakova, Katarina [2 ]
Sedlak, Milos [1 ]
机构
[1] Univ Pardubice, Inst Organ Chem & Technol, Fac Chem Technol, Studentska 573, Pardubice 53210, Czech Republic
[2] Univ Pardubice, Fac Chem Technol, Dept Biol & Biochem Sci, Studentska 573, Pardubice 53210, Czech Republic
来源
MONATSHEFTE FUR CHEMIE | 2017年 / 148卷 / 12期
关键词
Bioorganic chemistry; Drug research; Enzymes; Carbamates; Cholinesterase inhibitors; In vitro cytotoxicity; ACETYLCHOLINESTERASE INHIBITORS; ASYMMETRIC CYCLOPROPANATION; CARBAMATE DERIVATIVES; ALZHEIMERS-DISEASE; DRUG DISCOVERY; HALOGEN BONDS; COMPLEXES; DELIVERY; LIGANDS; DESIGN;
D O I
10.1007/s00706-017-2026-5
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
This present paper describes the preparation and characterization of a series of O-substituted N-cycloalkylcarbamate derivatives. These compounds were tested as inhibitors of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). All studied carbamates exhibited moderate inhibitory activity of both cholinesterases with values of IC50 in the range of 36.1-78.6 mu M for AChE and 9.8-215.4 mu M for BChE, respectively. These values are comparable with those values of inhibition obtained with the established drug rivastigmine. The cytotoxicity of all carbamates was evaluated using standard in vitro test with Jurkat cells. Many of the studied carbamates can be considered as promising compounds for potential medicinal applications with regard to their inhibitory activity as well as negligible cytotoxicity.
引用
收藏
页码:2143 / 2153
页数:11
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