Synthesis and Antidepressant and Anxiolytic Activity of 1,2,4,5-Tetrahydro-3H-Pyrrolo[1,2-a][1,4]Diazepin-3-ones

A series of new 1,2,4,5-tetrahydro-3 H -pyrrolo[1,2- a ][1,4]diazepin-3-one derivatives were synthesized from widely available furfurol, 3-aminopropionic acid, and amines. The antidepressant and anxiolytic properties of the obtained compounds were investigated. Results of Nomura and Porsolt forced s...

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Bibliographic Details
Published in:Pharmaceutical chemistry journal 2013-12, Vol.47 (9), p.464-469
Main Authors: Mokrov, G. V., Likhosherstov, A. M., Poseva, V. I., Molodavkin, G. M., Lezina, V. P., Gudasheva, T. A., Voronina, T. A.
Format: Article
Language:English
Subjects:
Medicine
Organic Chemistry
Pharmacology/Toxicology
Pharmacy
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Summary:A series of new 1,2,4,5-tetrahydro-3 H -pyrrolo[1,2- a ][1,4]diazepin-3-one derivatives were synthesized from widely available furfurol, 3-aminopropionic acid, and amines. The antidepressant and anxiolytic properties of the obtained compounds were investigated. Results of Nomura and Porsolt forced swimming tests showed that some of the compounds exhibited antidepressant activity at doses of 7 μmol/kg (1.1 – 2.2 mg/kg). Use of the Vogel conflict test showed that several compounds possessed anxiolytic activity at the same doses. The activities of the most active compounds exceeded those of the reference drugs, antidepressant amitriptyline and daily tranquilizer medazepam, at doses of 10 mg/kg.
ISSN:0091-150X
1573-9031
DOI:10.1007/s11094-013-0981-7