Activity profile of glycolamide ester prodrugs of ibuprofen.
Glycolamide esters of ibuprofen (I), namely, unsubstituted (II), N,N dimethyl (III), and N,N diethyl (IV), were synthesized and studied for different physicochemical, pharmacological, and toxicological properties. They were comparable with I in respect of anti-inflammatory and analgesic activity but did not exhibit reduction in the ulcerogenicity on oral administration. However, all three exhibited significantly better topical activity in carrageenan-induced rat paw edema assay. In the same assay, they provided significant protection against inflammation when applied at a site remote to the inflammation site.
College of Pharmacy, Pushp Vihar Sector 3, New Delhi 110 017, India.
A K
AK
Bansal
R K
RK
Khar
R
R
Dubey
A K
AK
Sharma
D000284:Administration, Oral; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D002351:Carrageenan / Q000008:administration & dosage; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy; D004952:Esters; D006016:Glycolates; D006801:Humans; D007052:Ibuprofen / Q000031:analogs & derivatives / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D007249:Inflammation; D008297:Male; D011355:Prodrugs; D051381:Rats; D017208:Rats, Wistar; D013276:Stomach Ulcer / Q000139:chemically induced* / Q000517:prevention & control
D000894:Anti-Inflammatory Agents, Non-Steroidal; D004952:Esters; D006016:Glycolates; D011355:Prodrugs; C053956:glycolamide; D002351:Carrageenan; D007052:Ibuprofen