Potent bradykinin B1 receptor antagonists: 4-substituted phenyl cyclohexanes.

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.

• Authors: Dai-Shi Su, John L Lim, M Kristine Markowitz, Bang-Lin Wan, Kathy L Murphy, Duane R Reiss, C Meacham Harrell, Stacy S O'Malley, Rick W Ransom, Raymond S L Chang, Douglas J Pettibone, Cuyue Tang, Thomayant Prueksaritanont, Roger M Freidinger, Mark G Bock
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 17 Issue 11 Pg. 3006-9 (Jun 01 2007) ISSN: 0960-894X [Print] England
• PMID: 17428657 (Publication Type: Journal Article)

Chemical References

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

Topics

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