The SAR studies of novel CB2 selective agonists, benzimidazolone derivatives.

Bioorg Med Chem Lett

Discovery Chemistry Research, Pfizer Global Research & Development, Nagoya Laboratories, Pfizer Japan Inc., 5-2 Taketoyo, Aichi 470-2393, Japan.

Published: June 2008

AI Article Synopsis

  • Scientists found new compounds called benzimidazolone derivatives that work specifically on a receptor in the body called CB2.
  • They studied these compounds to make them stronger and last longer in the body.
  • One compound, called Compound 39, showed great results by lasting long when tested and helping with pain in rats that had a specific condition.

Article 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.

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http://dx.doi.org/10.1016/j.bmcl.2008.04.032DOI Listing

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