Design, synthesis, and preliminary pharmacological evaluation of 1,4-diazabicyclo[4.3.0]nonan-9-ones as a new class of highly potent nootropic agents

Authors
Manetti, D Ghelardini, C Bartolini, A Bellucci, C Dei, S Galeotti, N Gualtieri, F Romanelli, MN Scapecchi, S Teodori, E
Citation
D. Manetti et al., Design, synthesis, and preliminary pharmacological evaluation of 1,4-diazabicyclo[4.3.0]nonan-9-ones as a new class of highly potent nootropic agents, J MED CHEM, 43(10), 2000, pp. 1969-1974
Citations number
27
Categorie Soggetti
Chemistry & Analysis
Journal title
JOURNAL OF MEDICINAL CHEMISTRY
ISSN journal
00222623 → ACNP
Volume
43
Issue
10
Year of publication
2000
Pages
1969 - 1974
Database
ISI
SICI code
0022-2623(20000518)43:10<1969:DSAPPE>2.0.ZU;2-L
Abstract
Several 4-substituted 1,4-diazabicyclo[4.3.0]nonan-9-ones have been synthes ized and tested in vivo on mouse passive avoidance test, to evaluate their nootropic activity. The results show that they represent a new class of noo tropic drugs with a pharmacological profile very similar to that of piracet am, showing much higher potency with respect to the reference. Among the co mpounds studied, 7 (DM 232) shows outstanding potency, being active at the dose of 0.001 mg kg(-1) sc.