Synthesis Under Microwave Irradiation and Molecular Docking of Some Novel Bioactive Thiadiazoles

Mini Rev Med Chem. 2019;19(5):437-447. doi: 10.2174/1389557518666180329122317.

Abstract

Background: A novel series of fused imidazole was prepared from the reaction of 2- bromoacetyl-3-phenyl-1,3,4-thiadiazole with various heterocyclic amines under microwave irradiation. The structures of all the novel products were elucidated based on the elemental analysis and spectral data.

Results: In addition, the biological activity of the newly synthesized compounds was evaluated and the results obtained indicate their potency as anti-inflammatory, analgesic and anti- ulcer agents.

Conclusion: The binding mechanism of the most active compounds was studied using MOE to analyze the molecular interactions.

Keywords: 1,3,4-thiadiazoles; analgesic and anti-ulcer agents; anti-inflammatory; fused imidazoles; heterocyclic amines; microwave irradiation..

MeSH terms

  • Analgesics / chemical synthesis
  • Analgesics / chemistry*
  • Analgesics / pharmacology
  • Analgesics / therapeutic use
  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / chemical synthesis
  • Anti-Inflammatory Agents, Non-Steroidal / chemistry*
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology
  • Anti-Inflammatory Agents, Non-Steroidal / therapeutic use
  • Anti-Ulcer Agents / chemical synthesis
  • Anti-Ulcer Agents / chemistry*
  • Anti-Ulcer Agents / pharmacology
  • Anti-Ulcer Agents / therapeutic use
  • Chemistry Techniques, Synthetic / methods
  • Cyclooxygenase 2 / metabolism
  • Edema / drug therapy
  • Edema / metabolism
  • Humans
  • Imidazoles / chemical synthesis
  • Imidazoles / chemistry
  • Imidazoles / pharmacology
  • Imidazoles / therapeutic use
  • Microwaves
  • Molecular Docking Simulation
  • Rats
  • Stomach Ulcer / drug therapy
  • Stomach Ulcer / metabolism
  • Thiadiazoles / chemical synthesis
  • Thiadiazoles / chemistry*
  • Thiadiazoles / pharmacology
  • Thiadiazoles / therapeutic use

Substances

  • Analgesics
  • Anti-Inflammatory Agents, Non-Steroidal
  • Anti-Ulcer Agents
  • Imidazoles
  • Thiadiazoles
  • Cyclooxygenase 2