Kinetics and mechanism of the enzymatic hydrolysis of aspirin phenylalanine ethyl ester

Discovery of a “True” Aspirin Prodrug

“…They usually have better aqueous stability than aspirin, making them potentially more suitable for a variety of pharmaceutical presentations . There has accordingly been a lot interest in the area in the past both as a drug development opportunity and because the design of a successful prodrug represents a significant and interesting scientific conundrum. , Reported aspirin derivatives include aspirin anhydride, benzodioxinone derivatives, acylal derivatives, N -(hydroxyalkyl) amides, 2-formylphenyl derivatives, straightforward alkyl and aryl esters, triglycerides for lipase targeting, acyloxyalkyl esters, sulfinyl and sulfonyl esters, phenylalanine amides, amino acid derivatives, indolediones as hypotoxic tissue targeting agents, and dual release mechanism prodrugs . Ideally, an aspirin prodrug should be stable under aqueous conditions and only undergo activation during the absorption and distribution process …”