58910-35-3Relevant academic research and scientific papers
Synthesis, biological activity evaluation and molecular modeling study on the new isoconessimine derivatives as acetylcholinesterase inhibitors
Jin, Guofei,Yang, Zhongduo,Xue, Weiwei,Sheng, Jie,Shi, Yin,Yao, Xiaojun
, p. 1228 - 1233 (2013)
New isoconessimine derivatives were synthesized from conessine (1) and evaluated as acetylcholinesterase (AChE) inhibitors. The derivatives were prepared via two reaction steps, N-demethylation and nucleophilic substitution. All of the synthesized derivatives exhibited more potential anti- acetylcholinesterase activities than conessine (1) (IC50=16 μmol·L-1) and isoconessimine (2) (IC50>300 μmol·L-1). Compound 7b (3β-[methyl-[2-(4-nitrophenoxy) ethyl]amino]con-5-enine) showed the most potent inhibitory activity with an IC50 of 110 nmol/L which is close to that of reference compound huperzine A (IC50=70 nmol/L). The mode of AChE inhibition by 7b was reversible and non-competitive. In addition, molecular modeling was performed to explore the binding mode of inhibitor 7b at the active site of AChE and the results showed that 7b could be docked into the acetylcholinesterase active site and compound 7b had hydrophobic interactions with Trp279 and Leu282. A series of 3-N-aryloxyethyl substitutional isoconessimine derivatives were synthesized and evaluated as acetylcholinesterase (AChE) inhibitors. All of the synthesized derivatives exhibited potential anti-acetylcholinesterase activities with IC50 values at micromolar to sub-micromolar range. 7b showed the most potent inhibitory activity with an IC50of 110 nmol/L. The molecular docking results showed that 7b can be well docked into the active site of acetylcholinesterase. Copyright
Choline derivatives brominated three ethyl-2 - (2,4-dinitrophenoxy) ethyl ammonium preparation method
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Paragraph 0018; 0023; 0024, (2016/10/07)
The invention discloses a preparation method of a choline derivative, namely, bromotriethyl-2-(2,4-dinitrophenoxyl)ethylammonium. The invention discloses a preparation method of a novel choline derivative. The preparation method comprises the following st
Synthesis and biological activity of KCB-328 and its analogues: Novel class III antiarrhythmic agents with little reverse frequency dependence
Kim, Dong-Ick,Kim, Hak-Yeop,Kwon, Lae-Sung,Park, Sung-Dae,Jeon, Gee-Ho,Jung, Kyung-Yun,Min, Jae-Ki,Nam, Woong-Hyun,Lee, Kiho,Chung, You-Sup,Tanabe, Shigeru,Kozono, Toshiro
, p. 85 - 90 (2007/10/03)
A series of 3,4-dimethoxyphenethylamine derivatives was prepared, and their prolongation effects on effective refractory period of contractile response (ERPc) and action potential duration (APD) in isolated guinea-pig papillary muscles at 1 Hz and 3 Hz were examined. SAR studies led to the identification of KCB-328 (51) which is a novel class III antiarrhythmic agent with little reverse frequency dependence.
