3-Arylsulphonyl-5-arylamino-1,3,4-thiadiazol-2(3H)ones as anti-inflammatory and analgesic agents

Bioorg Med Chem. 2001 Aug;9(8):2149-53. doi: 10.1016/s0968-0896(01)00121-3.

Abstract

Two series of 3-arylsulphonyl-5-arylamino-1,3,4-thiadiazol-2(3H)ones 2 with potential anti-inflammatory and analgesic activity were prepared and tested. Pharmacological results revealed that all the title compounds, endowed with an arylsulphonyl side chain, possess good antalgic activity and fair anti-inflammatory properties. The analgesic profile of the two series, evaluated by the acetic acid writhing test, showed that compounds 2c, 2f and 2h, in particular, were the most active. Structure-activity relationships are briefly discussed.

MeSH terms

  • Analgesics / chemical synthesis*
  • Analgesics / chemistry
  • Analgesics / therapeutic use
  • Animals
  • Anti-Inflammatory Agents / chemical synthesis*
  • Anti-Inflammatory Agents / chemistry
  • Anti-Inflammatory Agents / therapeutic use
  • Disease Models, Animal
  • Edema / drug therapy
  • Female
  • Male
  • Mice
  • Pain / drug therapy
  • Rats
  • Sulfur Compounds / chemical synthesis*
  • Sulfur Compounds / chemistry
  • Thiazoles / chemical synthesis*
  • Thiazoles / chemistry
  • Thiazoles / pharmacology

Substances

  • Analgesics
  • Anti-Inflammatory Agents
  • Sulfur Compounds
  • Thiazoles