Journal of medicinal and pharmaceutical chemistry 2011-04-14

Synthesis and biological evaluation of 3,7-diazabicyclo[4.3.0]nonan-8-ones as potential nootropic and analgesic drugs.

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

Index: J. Med. Chem. 54 , 2512-6, (2011)

Full Text: HTML

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.