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Coumarin-based prodrugs 2. Synthesis and bioreversibility studies of an esterase-sensitive cyclic prodrug of dadle, an opioid peptide

✍ Scribed by Binghe Wang; Wei Wang; Huijuan Zhang; Daxian Shan; Terrill D. Smith


Book ID
104364672
Publisher
Elsevier Science
Year
1996
Tongue
English
Weight
245 KB
Volume
6
Category
Article
ISSN
0960-894X

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✦ Synopsis


A coumarin-based esterase-sensitive cyclic prodrug of an opioid peptide, DADLE, was prepared. The cyclic prodrug quickly released (tl/2 = 761 min) its original peptide, DADLE, upon esterase catalyzed hydrolysis. Such a system can be used for the preparation of cyclic prodrugs of other biologically active peptides aimed at improving their bioavailability.


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