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Prodrugs of prostate specific membrane antigen (PSMA) inhibitor

Authors: Slusher, B.; Rais, R.; Krečmerová, M. (Marcela); Tichý, T. (Tomáš); Majer, P. (Pavel); Jančařík, A. (Andrej);

Prodrugs of prostate specific membrane antigen (PSMA) inhibitor

Abstract

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.

Country
Czech Republic
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Keywords

POM, isopropyloxycarbonyloxymethyl, 2-Phosphonomethylpentanedioic acid (2-PMPA), PSMA, glutamate carboxypeptidase II, prodrug, GCPII, pivaloyloxymethyl, POC

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selected citations
These citations are derived from selected sources.
This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Citations provided by BIP!
popularity
This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.
BIP!Popularity provided by BIP!
influence
This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Influence provided by BIP!
impulse
This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.
BIP!Impulse provided by BIP!
0
Average
Average
Average
Green
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