Antiinflammatory and antiproteolytic activities of newer indolyl isoquinolines.
Several indolyl isoquinoline derivatives were synthesized and evaluated for their antiinflammatory and antiproteolytic activities. These derivatives possessed 9.2-32.4% inhibition at a dose of 100 mg/kg i.p. against carrageenin-induced oedema. Four of these derivatives (IVb, IVd, IVe and IVk) exhibited high potency in inhibiting oedema. The degree of inhibition of trypsin-induced hydrolysis of bovine serum albumin, in vitro, by compounds IVb, IVd, IVe, IVi, IVj, IVk and IVl ranged from 10-42% at a final concentration of 1 mmol/l. In addition, these agents exhibited relatively non-toxic nature and their approx. LD50 was greater than 1000 mg/kg i.p.
D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis*; D002351:Carrageenan; D004487:Edema / Q000139:chemically induced / Q000503:physiopathology; D007546:Isoquinolines / Q000138:chemical synthesis* / Q000494:pharmacology; D007928:Lethal Dose 50; D051379:Mice; D011480:Protease Inhibitors / Q000138:chemical synthesis*; D051381:Rats; D014361:Trypsin Inhibitors / Q000138:chemical synthesis
D000893:Anti-Inflammatory Agents; D007546:Isoquinolines; D011480:Protease Inhibitors; D014361:Trypsin Inhibitors; D002351:Carrageenan