New 1,8-naphthyridine and quinoline derivatives as CB2 selective agonists.
A series of new 1,8-naphthyridine and quinoline derivatives were synthesized and evaluated for their cannabinoid receptor affinity. In particular, compounds 2, 5, 11, and 13 showed a high CB(2) affinity and CB(2) versus CB(1) selectivity, in agreement with molecular modeling studies. Furthermore, compound 2 also exhibited in vivo antinociceptive effects.
Manera
Clementina
C
Dipartimento di Scienze Farmaceutiche, Università di Pisa, Via Bonanno 6, 56126 Pisa, Italy. manera@farm.unipi.it
Cascio
Maria Grazia
MG
Benetti
Veronica
V
Allarà
Marco
M
Tuccinardi
Tiziano
T
Martinelli
Adriano
A
Saccomanni
Giuseppe
G
Vivoli
Elisa
E
Ghelardini
Carla
C
Di Marzo
Vincenzo
V
Ferrarini
Pier Luigi
PL
D000818:Animals; D002460:Cell Line; D006801:Humans; D051379:Mice; D009287:Naphthyridines / Q000737:chemistry* / Q000494:pharmacology; D010147:Pain Measurement / Q000187:drug effects / Q000379:methods; D011804:Quinolines / Q000737:chemistry* / Q000494:pharmacology; D043884:Receptor, Cannabinoid, CB1 / Q000819:agonists / Q000096:biosynthesis / Q000235:genetics / Q000502:physiology; D043885:Receptor, Cannabinoid, CB2 / Q000819:agonists* / Q000096:biosynthesis / Q000235:genetics / Q000502:physiology
D009287:Naphthyridines; D011804:Quinolines; D043884:Receptor, Cannabinoid, CB1; D043885:Receptor, Cannabinoid, CB2