Novel benzimidazole derivatives as selective CB2 agonists.
The preparation and evaluation of a novel class of CB2 agonists based on a benzimidazole moiety are reported. They showed binding affinities up to 1nM towards the CB2 receptor with partial to full agonist potencies. They also demonstrated good to excellent selectivity (>1000-fold) over the CB1 receptor.
Pagé
Daniel
D
Department of Medicinal Chemistry, AstraZeneca R&D Montréal, 7171 Frederick-Banting, St-Laurent, Que., Canada. daniel.page@astrazeneca.com
Balaux
Elise
E
Boisvert
Luc
L
Liu
Ziping
Z
Milburn
Claire
C
Tremblay
Maxime
M
Wei
Zhongyong
Z
Woo
Simon
S
Luo
Xuehong
X
Cheng
Yun-Xing
YX
Yang
Hua
H
Srivastava
Sanjay
S
Zhou
Fei
F
Brown
William
W
Tomaszewski
Miroslaw
M
Walpole
Christopher
C
Hodzic
Leila
L
St-Onge
Stéphane
S
Godbout
Claude
C
Salois
Dominic
D
Payza
Kemal
K
Payza
Keymal
K
D001562:Benzimidazoles / Q000138:chemical synthesis / Q000737:chemistry*; D001667:Binding, Competitive; D063385:Cannabinoid Receptor Modulators / Q000737:chemistry; D002186:Cannabinoids / Q000737:chemistry; D002626:Chemistry, Pharmaceutical / Q000379:methods; D015195:Drug Design; D006801:Humans; D008956:Models, Chemical; D043884:Receptor, Cannabinoid, CB1 / Q000737:chemistry; D043885:Receptor, Cannabinoid, CB2 / Q000737:chemistry*; D043882:Receptors, Cannabinoid / Q000737:chemistry; D013329:Structure-Activity Relationship; D013678:Technology, Pharmaceutical / Q000379:methods
D001562:Benzimidazoles; D063385:Cannabinoid Receptor Modulators; D002186:Cannabinoids; D043884:Receptor, Cannabinoid, CB1; D043885:Receptor, Cannabinoid, CB2; D043882:Receptors, Cannabinoid; C031000:benzimidazole