Substituted coumarins as esterase-sensitive prodrug moieties with improved release rates.
Our laboratory has recently reported a coumarin-based prodrug system for the preparation of esterase-sensitive prodrugs of amines, peptides, and peptidomimetics. However, the release from this prodrug system was undesirably slow for some drug moieties. In this report, we describe the synthesis and evaluation of several substituted coumarin-based prodrugs of model amines with significantly increased release rates.
Department of Chemistry, North Carolina State University, Raleigh 27695-8204, USA.
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Y
Liao
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Wang
D000818:Animals; D001682:Biological Availability; D003374:Coumarins / Q000138:chemical synthesis* / Q000737:chemistry* / Q000493:pharmacokinetics; D004950:Esterases / Q000378:metabolism* / Q000493:pharmacokinetics; D007700:Kinetics; D011355:Prodrugs / Q000737:chemistry*; D013552:Swine; D013997:Time Factors
D003374:Coumarins; D011355:Prodrugs; C030123:coumarin; D004950:Esterases