- The SAR studies of novel CB2 selective agonists, benzimidazolone derivatives.
The SAR studies of novel CB2 selective agonists, benzimidazolone derivatives.
Bioorganic & medicinal chemistry letters (2008-04-29)
Hirofumi Omura, Makoto Kawai, Akiko Shima, Yasuhiro Iwata, Fumitaka Ito, Tsutomu Masuda, Atsuko Ohta, Naoya Makita, Kiyoyuki Omoto, Hiromi Sugimoto, Akira Kikuchi, Hiroshi Iwata, Kazuo Ando
PMID18440813
ABSTRAKT
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.
MATERIAŁY