Newer indolyl imidazolones as anti-inflammatory agents.
Sixteen new 1,2-disubstituted-4-(indol-3'-yl)methylene imidazol-5-ones were synthesized by the condensation of oxazolone with different aryl amines and evaluated as to their anti-inflammatory and antiproteolytic activities. These derivatives showed 2-38% protection against carrageenin-induced paw oedema in albino rats at a dose of 100 mg/kg p.o. All compounds showed antiproteolytic activity. The degree of inhibition against trypsin-induced hydrolysis of casein ranged from 10 to 75% at a concentration of 4 X 10(-4) mol/l. Furthermore, active compounds of the series were also screened for their analgesic activity against aconitine-induced writhing in albino mice. The toxicity of the compounds was reflected by their approximate LD50 values.
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000633:toxicity; D002364:Caseins; D004487:Edema / Q000517:prevention & control; D005260:Female; D006868:Hydrolysis; D007093:Imidazoles / Q000494:pharmacology* / Q000633:toxicity; D007211:Indoles / Q000494:pharmacology* / Q000633:toxicity; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D010437:Peptic Ulcer / Q000139:chemically induced; D051381:Rats; D014361:Trypsin Inhibitors
D000894:Anti-Inflammatory Agents, Non-Steroidal; D002364:Caseins; D007093:Imidazoles; D007211:Indoles; D014361:Trypsin Inhibitors