The SAR studies of novel CB2 selective agonists, benzimidazolone derivatives.
Benzimidazolone derivatives were discovered as novel CB2 selective agonists. Structure Activity Relationship (SAR) studies around them were examined to improve metabolic stability. Compound 39 exhibited excellent metabolic stability in human liver microsomes (HLM) and significant attenuation of the chronic colonic allodynia in the TNBS-treated rats by po administration.
Omura
Hirofumi
H
Discovery Chemistry Research, Pfizer Global Research & Development, Nagoya Laboratories, Pfizer Japan Inc., 5-2 Taketoyo, Aichi 470-2393, Japan. omurah@gmail.com
Kawai
Makoto
M
Shima
Akiko
A
Iwata
Yasuhiro
Y
Ito
Fumitaka
F
Masuda
Tsutomu
T
Ohta
Atsuko
A
Makita
Naoya
N
Omoto
Kiyoyuki
K
Sugimoto
Hiromi
H
Kikuchi
Akira
A
Iwata
Hiroshi
H
Ando
Kazuo
K
D000818:Animals; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D020650:Combinatorial Chemistry Techniques; D015195:Drug Design; D006801:Humans; D015394:Molecular Structure; D051381:Rats; D043884:Receptor, Cannabinoid, CB1 / Q000819:agonists; D043885:Receptor, Cannabinoid, CB2 / Q000819:agonists*; D013329:Structure-Activity Relationship
D001562:Benzimidazoles; D043884:Receptor, Cannabinoid, CB1; D043885:Receptor, Cannabinoid, CB2; C014353:benzimidazolone