Potent bradykinin B1 receptor antagonists: 4-substituted phenyl cyclohexanes

Bioorg Med Chem Lett. 2007 Jun 1;17(11):3006-9. doi: 10.1016/j.bmcl.2007.03.059. Epub 2007 Mar 21.

Abstract

Selective bradykinin (BK) B(1) receptor antagonists have been shown to be antinociceptive in animal models and could be novel therapeutic agents for the treatment of pain and inflammation. Elucidation of the structure-activity relationships of the biphenyl moiety of the lead compound 1 provided a potent new structural class of BK B(1) receptor antagonists.

MeSH terms

  • Analgesics / chemical synthesis
  • Analgesics / chemistry*
  • Analgesics / pharmacology
  • Animals
  • Animals, Genetically Modified
  • Anti-Inflammatory Agents, Non-Steroidal / chemical synthesis
  • Anti-Inflammatory Agents, Non-Steroidal / chemistry*
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology
  • Bradykinin B1 Receptor Antagonists*
  • Cyclohexanes / chemical synthesis
  • Cyclohexanes / chemistry*
  • Cyclohexanes / pharmacology
  • Humans
  • Hydrocarbons, Fluorinated / chemical synthesis
  • Hydrocarbons, Fluorinated / chemistry*
  • Hydrocarbons, Fluorinated / pharmacology
  • Pyridines / chemical synthesis
  • Pyridines / chemistry*
  • Pyridines / pharmacology
  • Rats
  • Receptor, Bradykinin B1 / genetics
  • Structure-Activity Relationship

Substances

  • Analgesics
  • Anti-Inflammatory Agents, Non-Steroidal
  • Bradykinin B1 Receptor Antagonists
  • Cyclohexanes
  • Hydrocarbons, Fluorinated
  • Pyridines
  • Receptor, Bradykinin B1