N-trifluoroacetyl derivatives as pharmacological agents. V. Evaluation of antiinflammatory and antimicrobial activities of some N-heterocyclic trifluoroacetamides

Farmaco. 1990 Feb;45(2):223-35.

Abstract

Following the investigation on pharmacological aspects of N-trifluoroacetyl compounds some heterocyclic trifluoroacetamides were prepared and explored as potential antiinflammatory-analgesic and antimicrobial agents. The trifluoroacetamides 3, 4, 5, and 6 reached significant activity in the hot plate analgesic test; the same 4 and 5, along with 7 and 8 showed inhibitory properties in the adjuvant arthritis test; only 7 however, displayed a significant dose-dependent activity in the carrageenin edema test. In addition the parent heterocyclic amines were similarly explored for comparison. Test for antimicrobial activity were carried out in parallel. Among the examined compounds, only 4-aminomorpholine and 2-aminobenzimidazole were found active when assayed against gram+ and gram- bacteria and mycetes.

MeSH terms

  • Animals
  • Anti-Bacterial Agents / chemical synthesis*
  • Anti-Bacterial Agents / pharmacology
  • Anti-Bacterial Agents / toxicity
  • Anti-Inflammatory Agents, Non-Steroidal / chemical synthesis*
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology
  • Anti-Inflammatory Agents, Non-Steroidal / toxicity
  • Arthritis, Experimental / drug therapy
  • Bacteria / drug effects*
  • Edema / chemically induced
  • Edema / drug therapy
  • Fluoroacetates*
  • Heterocyclic Compounds / chemical synthesis*
  • Heterocyclic Compounds / pharmacology
  • Heterocyclic Compounds / toxicity
  • Male
  • Mice
  • Microbial Sensitivity Tests
  • Pain Measurement
  • Rats
  • Rats, Inbred Strains
  • Stomach Ulcer / chemically induced
  • Trifluoroacetic Acid / chemical synthesis
  • Trifluoroacetic Acid / pharmacology
  • Trifluoroacetic Acid / toxicity

Substances

  • Anti-Bacterial Agents
  • Anti-Inflammatory Agents, Non-Steroidal
  • Fluoroacetates
  • Heterocyclic Compounds
  • Trifluoroacetic Acid