Synthesis and Pharmacological Activity of 2-(Diethylamino)Ethyl 9-Hydroxy-9H-Fluorene-9-Carboxylate Hydrochloride

摘要

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.