New fluorenecarboxylic acid derivatives (structural analogs of amizil) were synthesized. A compound with low toxicity (LD50 = 45 ± 9.9 mg/kg) and antidepressant and antianxiety effects was identified. The central and peripheral muscarinic anticholinergic properties of 2-dimethylaminoethyl 9-hydroxyfluorene-9-carboxylate were studied using an arecoline tremor model. Apharmacological analysis showed that the new amizil structural analog exhibited pronounced central muscarinic anticholinergic activity and did not possess peripheral muscarinic anticholinergic effects. The advantages of the tested compound over amizil, amitriptyline that is widely used in the clinic, and the benzodiazepine tranquilizer diazepam were discussed. The results indicated that 2-diethylaminoethyl 9-hydroxyfluorene-9-carboxylate was promising for further development for the treatment of depressive and anxiety disorders.

中文翻译：

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2-(二乙氨基)乙基9-羟基-9H-芴-9-羧酸盐酸盐的合成及药理活性

合成了新的芴羧酸衍生物（amizil 的结构类似物）。确定了一种具有低毒性 (LD50 = 45 ± 9.9 mg/kg) 和抗抑郁和抗焦虑作用的化合物。使用槟榔碱震颤模型研究了 2-二甲氨基乙酯 9-羟基芴-9-羧酸的中枢和外周毒蕈碱抗胆碱能特性。A药理学分析表明，新的amizil结构类似物表现出明显的中枢毒蕈碱抗胆碱能活性，并且不具有外周毒蕈碱抗胆碱能作用。讨论了供试化合物相对于临床上广泛使用的阿米齐尔、阿米替林和苯二氮卓类镇静剂地西泮的优势。