Investigations on the synthesis and pharmacological properties of N-substituted derivatives of 4-alkoxy-6-methyl-1H-pyrrolo[3,4-c]pyridine-1,3(2H)-diones

Farmaco. 2005 Jan;60(1):53-9. doi: 10.1016/j.farmac.2004.08.011. Epub 2004 Dec 19.

Abstract

Synthesis of N-substituted derivatives of 4-alkoxy-6-methyl-1H-pyrrolo[3,4-c]pyridine-1,3(2H)-diones (10-14, 18-21) is described. In the "writhing syndrome" test all compounds studied exhibited potent analgesic activity which was superior than that of acetylsalicylic acid. In the "hot plate" test imides 10, 12, 13, 18-20 acted also stronger than aspirin. Furthermore all compounds tested significantly suppressed the spontaneous locomotor activity of mice and prolonged barbiturate sleep of these animals.

MeSH terms

  • Analgesia*
  • Analgesics / chemical synthesis*
  • Analgesics / chemistry
  • Analgesics / pharmacology
  • Animals
  • Lethal Dose 50
  • Male
  • Mice
  • Motor Activity / drug effects
  • Pyrroles / chemical synthesis*
  • Pyrroles / chemistry*
  • Pyrroles / pharmacology
  • Structure-Activity Relationship

Substances

  • Analgesics
  • Pyrroles