Investigations on the 4-Quinolone-3-Carboxylic Acid Motif Part 5: Modulation of the Physicochemical Profile of a Set of Potent and Selective Cannabinoid-2 Receptor Ligands through a Bioisosteric Approach (pages 920–934)
Dr. Claudia Mugnaini, Stefania Nocerino, Valentina Pedani, Dr. Serena Pasquini, Prof. Andrea Tafi, Maria De Chiaro, Dr. Luca Bellucci, Prof. Massimo Valoti, Dr. Francesca Guida, Dr. Livio Luongo, Dr. Stefania Dragoni, Dr. Alessia Ligresti, Dr. Avraham Rosenberg, Dr. Daniele Bolognini, Dr. Maria Grazia Cascio, Prof. Roger G. Pertwee, Dr. Ruin Moaddel, Prof. Sabatino Maione, Dr. Vincenzo Di Marzo and Prof. Federico Corelli
Article first published online: 2 MAR 2012 | DOI: 10.1002/cmdc.201100573
Less psycho more active! Cannabinoid receptor type 2 (CB2)-selective agonists have potential as therapeutics for the treatment of pain, however, poor selectivity over CB1 has hampered the development. Here, the modulation of physicochemical properties of CB2 ligands through a simple bioisosteric approach was performed without significant loss of receptor affinity in an attempt to obtain potent leads with desirable drug-like properties.