- Synthesis and biological evaluation of 3,7-diazabicyclo[4.3.0]nonan-8-ones as potential nootropic and analgesic drugs.
Synthesis and biological evaluation of 3,7-diazabicyclo[4.3.0]nonan-8-ones as potential nootropic and analgesic drugs.
Journal of medicinal chemistry (2011-03-09)
Elisabetta Martini, Lorenzo Di Cesare Mannelli, Gianluca Bartolucci, Carlo Bertucci, Silvia Dei, Carla Ghelardini, Luca Guandalini, Dina Manetti, Serena Scapecchi, Elisabetta Teodori, Maria Novella Romanelli
PMID21381762
ABSTRACT
A series of cis and trans 3,7-diazabicyclo[4.3.0]nonan-8-ones has been synthesized and tested for their ability to revert scopolamine-induced amnesia in the mouse passive-avoidance test. The racemates of the most potent compounds 4 and 7 were separated and tested, but no enantioselectivity was found for the nootropic activity. Compounds 4 and 7 and their enantiomers displayed interesting antihyperalgesic activity in two models of neuropathic pain (streptozotocin-induced and oxalilplatin-induced neuropathy) in comparison with pregabalin.
MATERIALS
Product Number
Brand
Product Description
Sigma-Aldrich
L-Ascorbic acid, puriss. p.a., ACS reagent, reag. ISO, Ph. Eur., 99.7-100.5% (oxidimetric)