Activity profile of glycolamide ester prodrugs of ibuprofen

Glycolamide esters of ibuprofen (I), namely, unsubstituted (II), N,N dimeth yl (III), and N,N diethyl (N), were synthesized and studied for different p hysicochemical, pharmacological, and toxicological properties. They were co mparable with 1 in respect of anti-inflammatory and analgesic activity but did not exhibit reduction in the ulcerogenicity on oral administration Howe ver all three exhibited significantly better topical activity in carrageena n-induced rat paw edema assay. In the same assay,they provided significant protection against inflammation when applied at a site remote to the inflam mation site.