Chemical feasibility studies of a potential coumarin-based prodrug system

DOI: 10.1016/0960-894X(96)00147-3

Source and publish data:

Bioorganic and Medicinal Chemistry Letters p. 945 - 950 (1996)

Update date:2022-08-05

Topics:

Authors:

Wang, Binghe

Zhang, Huijuan

Wang, Wei

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Article abstract of DOI:10.1016/0960-894X(96)00147-3

By using model amines, several amides of coumarinic acid with the phenolic hydroxyl group protected as an ester were prepared. These model amides underwent a facile (t( 1/2 ) 1.5-31 min) lactonization to release the original amine compounds upon esterase catalyzed hydrolysis of the phenolic ester. Such a system can be used for the preparation of esterase-sensitive prodrugs of amine-containing compounds or peptids.

Full text of DOI:10.1016/0960-894X(96)00147-3

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