Substituted coumarins as esterase-sensitive prodrug moieties with improvedrelease rates

Our laboratory has recently reported a coumarin-based prodrug system for th e preparation of esterase-sensitive prodrugs of amines, peptides, and pepti domimetics. However, the release from this prodrug system was undesirably s low for some drug moieties. In this report, we describe the synthesis and e valuation of several substituted coumarin-based prodrugs of model amines wi th significantly increased release rates. (C) 1999 Elsevier Science Ltd. Al l rights reserved.