Synthesis and antiinflammatory activity of some 2-(substituted-pyridinyl)benzimidazoles

J Med Chem. 1980 Jul;23(7):734-8. doi: 10.1021/jm00181a007.

Abstract

A series of 2-(2-pyridinyl)benzimidazoles was synthesized and evaluated for antiinflammatory activity by the carrageenan-induced rat paw edema assay. Among several active derivatives, 2-(5-ethylpyridin-2-yl)benzimidazole (6) was selected for further study. A comparison of compound 6 with phenylbutazone and tiaramide revealed that 6 possesses stronger activity in acute inflammatory models possibly with slightly less gastrointestinal irritation than both phenylbutazone and tiaramide.

MeSH terms

  • Animals
  • Anti-Inflammatory Agents / chemical synthesis*
  • Anti-Inflammatory Agents, Non-Steroidal / chemical synthesis
  • Benzimidazoles / chemical synthesis*
  • Benzimidazoles / pharmacology
  • Cyclooxygenase Inhibitors
  • Edema / drug therapy
  • Mice
  • Rats
  • Solubility
  • Stomach Ulcer / chemically induced
  • Structure-Activity Relationship

Substances

  • Anti-Inflammatory Agents
  • Anti-Inflammatory Agents, Non-Steroidal
  • Benzimidazoles
  • Cyclooxygenase Inhibitors