
handle: 11104/0293187
Various structural types of prodrugs of 2-phosphonomethylpentanedioic acid were synthesized as GCPII inhibitors. The prodrug with the optimal pharmacokinetic profile was obtained by introducing POC groups on both the phosphonate and α-carboxylate. Thus formed Tris-POC-2-PMPA afforded excellent release of parent 2-PMPA following oral administration in both mice and dog.
POM, isopropyloxycarbonyloxymethyl, 2-Phosphonomethylpentanedioic acid (2-PMPA), PSMA, glutamate carboxypeptidase II, prodrug, GCPII, pivaloyloxymethyl, POC
POM, isopropyloxycarbonyloxymethyl, 2-Phosphonomethylpentanedioic acid (2-PMPA), PSMA, glutamate carboxypeptidase II, prodrug, GCPII, pivaloyloxymethyl, POC
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