208402-14-6Relevant articles and documents
Two new improved approaches to the synthesis of coumarin-based prodrugs
Zheng, Ailian,Wang, Wei,Zhang, Huijuan,Wang, Binghe
, p. 4237 - 4254 (2007/10/03)
Our laboratory has recently reported the development of a coumarin- based, esterase-sensitive prodrug system for the preparation of prodrugs of amines, peptides, and peptidomimetics. Biological evaluations including animal studies have demonstrated the cl
Chemical feasibility studies of a potential coumarin-based prodrug system
Wang, Binghe,Zhang, Huijuan,Wang, Wei
, p. 945 - 950 (2007/10/03)
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.