Syntheses and anticholinesterase activity of tetrahydrobenzazepine carbamates.
Syntheses and anticholinesterase activity of tetrahydrobenzazepine carbamates.
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四氢苯并氮杂氨基甲酸酯的合成和抗胆碱酯酶活性。
DOI：
10.1002/chin.199450166
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发表时间：
1994
影响因子：
7.3
通讯作者：
S. Jones
中科院分区：
文献类型：
--
作者：
Y. L. Chen;D. Liston;J. Nielsen;D. Chapin;A. Dunaiskis;K. Hedberg;J. Ives;J. Johnson;S. Jones
报道了一系列1,5-甲烷-2,3,4,5-四氢- 1h -2-苯并氮平-7-醇烷基氨基甲酸酯的合成。这些化合物中有许多是有效的乙酰胆碱酯酶（AChE）抑制剂。本文描述了这一系列化合物的体外AChE抑制、胆碱能作用、急性毒性和体内脑乙酰胆碱水平的升高。在小鼠被动回避实验中，具有代表性的化合物1d （5.6 mg/kg, po）能够逆转半钴-3诱导的健忘症。
The synthesis of a series of alkylcarbamates of 1,5-methano-2,3,4,5-tetrahydro-1H-2-benzazepin-7-ol is reported. Many of these compounds are potent acetylcholinesterase (AChE) inhibitors. The in vitro AChE inhibition, cholinergic effects, acute toxicity, and elevation of brain acetylcholine levels in vivo of this series of compounds are described. A representative compound, 1d (5.6 mg/kg, po), was able to reverse hemicolinium-3-induced amnesia in the mouse passive avoidance assay.