title: The SAR studies of novel CB2 selective agonists, benzimidazolone derivatives.
abstract: 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.
authors.affiliation: Discovery Chemistry Research, Pfizer Global Research & Development, Nagoya Laboratories, Pfizer Japan Inc., 5-2 Taketoyo, Aichi 470-2393, Japan. omurah@gmail.com
authors.forename: Hirofumi
authors.initials: H
authors.lastname: Omura
authors.forename: Makoto
authors.initials: M
authors.lastname: Kawai
authors.forename: Akiko
authors.initials: A
authors.lastname: Shima
authors.forename: Yasuhiro
authors.initials: Y
authors.lastname: Iwata
authors.forename: Fumitaka
authors.initials: F
authors.lastname: Ito
authors.forename: Tsutomu
authors.initials: T
authors.lastname: Masuda
authors.forename: Atsuko
authors.initials: A
authors.lastname: Ohta
authors.forename: Naoya
authors.initials: N
authors.lastname: Makita
authors.forename: Kiyoyuki
authors.initials: K
authors.lastname: Omoto
authors.forename: Hiromi
authors.initials: H
authors.lastname: Sugimoto
authors.forename: Akira
authors.initials: A
authors.lastname: Kikuchi
authors.forename: Hiroshi
authors.initials: H
authors.lastname: Iwata
authors.forename: Kazuo
authors.initials: K
authors.lastname: Ando
mesh_terms: 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
chemical_list: D001562:Benzimidazoles; D043884:Receptor, Cannabinoid, CB1; D043885:Receptor, Cannabinoid, CB2; C014353:benzimidazolone