N-trifluoroacetyl derivatives as pharmacological agents. V. Evaluation of antiinflammatory and antimicrobial activities of some N-heterocyclic trifluoroacetamides.
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.
Vigorita
M G
MG
Dipartimento Farmaco-Chimico facoltà di Farmacia, Università di Messina, Italy.
Previtera
T
T
Zappalà
C
C
Trovato
A
A
Monforte
M T
MT
Barbera
R
R
Pizzimenti
F
F
D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D001169:Arthritis, Experimental / Q000188:drug therapy; D001419:Bacteria / Q000187:drug effects*; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy; D005463:Fluoroacetates; D006571:Heterocyclic Compounds / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D008297:Male; D051379:Mice; D008826:Microbial Sensitivity Tests; D010147:Pain Measurement; D051381:Rats; D011919:Rats, Inbred Strains; D013276:Stomach Ulcer / Q000139:chemically induced; D014269:Trifluoroacetic Acid / Q000138:chemical synthesis / Q000494:pharmacology / Q000633:toxicity
D000900:Anti-Bacterial Agents; D000894:Anti-Inflammatory Agents, Non-Steroidal; D005463:Fluoroacetates; D006571:Heterocyclic Compounds; D014269:Trifluoroacetic Acid