Studies on synthesis and pharmacological activities of 1,2,4-triazolo[3,4-b]1,3,4-thiadiazoles and their dihydro analogues

Arch Pharm (Weinheim). 2009 Apr;342(4):210-22. doi: 10.1002/ardp.200800073.

Abstract

4-Amino-5-substituted aryl-3-mercapto-1,2,4-triazoles are versatile synthons for constructing various biologically active heterocycles. Starting from 4-amino-5-substituted aryl-3-mercapto-1,2,4-triazole 3a-c, a series of new 3,5-disubstituted-1,2,4-triazolo-[3,4-b]1,3,4-thiadiazoles and their 5,6-dihydrotriazolothiadiazoles were prepared. The structures of all the newly synthesized compounds have been confirmed by elemental analysis, IR,( 1)H-NMR, (13)C-NMR, and mass spectra. The antimicrobial effects of the synthesized compounds were investigated using the paper disc method. Anti-inflammatory and analgesic activities of the synthesized compounds were assessed by carrageenan-induced rat paw oedema method and by Eddy's hot plate method, respectively. Some of the compounds exhibited promising antimicrobial activities as well as moderate to good anti-inflammatory activity and analgesic activity.

MeSH terms

  • Analgesics, Non-Narcotic / chemical synthesis
  • Analgesics, Non-Narcotic / pharmacology
  • Animals
  • Anti-Infective Agents / chemical synthesis*
  • Anti-Infective Agents / pharmacology*
  • Anti-Inflammatory Agents, Non-Steroidal / chemical synthesis*
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
  • Bacteria / drug effects
  • Carrageenan
  • Edema / chemically induced
  • Edema / prevention & control
  • Female
  • Fungi / drug effects
  • Magnetic Resonance Spectroscopy
  • Male
  • Mass Spectrometry
  • Mice
  • Microbial Sensitivity Tests
  • Pain Measurement / drug effects
  • Rats
  • Rats, Wistar
  • Spectrophotometry, Infrared
  • Thiadiazoles / chemical synthesis*
  • Thiadiazoles / pharmacology*

Substances

  • Analgesics, Non-Narcotic
  • Anti-Infective Agents
  • Anti-Inflammatory Agents, Non-Steroidal
  • Thiadiazoles
  • Carrageenan