Glycerides as prodrugs. 3. Synthesis and antiinflammatory activity of [1-(p-chlorobenzoyl)-5-methoxy-2-methylindole-3-acetyl]glycerides (indomethacin glycerides)

Publisher Website
Google Scholar
Abstract
Mono-, bis-, and tris[1-(p-chlorobenzoyl)-5-methoxy-2-methylindole-3-acetyl]glycerides and 1,3-dialkanoyl-2-[1-(p-chlorobenzoyl)-5-methoxy-2-methylindole-3-acetyl]glycerides were synthesized and evaluated for antiinflammatory activity in the rat paw carrageenin edema assay. Three of the most active compounds were tested in the rat adjuvant arthritis model and found to be essentially equivalent in activity to indomethacin. On a molar basis, the acute gastric irritating properties of 2 of these compounds were 7-8 times less than indomethacin, resulting in a 2.5- to 3-fold improvement in the ratio of antiedema activity to ulcerogenicity.

This publication has 0 references indexed in Scilit: