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Drug development and industrial pharmacy

Activity profile of glycolamide ester prodrugs of ibuprofen.


PMID 11247537

Abstract

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.

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480959
Glycolamide, 98%
C2H5NO2