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Bioorg Med Chem Lett. 2010 Dec 15;20(24):7222-5. doi: 10.1016/j.bmcl.2010.10.109. Epub 2010 Oct 26.

The discovery and structure-activity relationships of indole-based inhibitors of glutamate carboxypeptidase II.

Author information

1
Eisai Research Institute, Baltimore, MD 21224, USA.

Abstract

A series of N-substituted 3-(2-mercaptoethyl)-1H-indole-2-carboxylic acids were synthesized as inhibitors of glutamate carboxypeptidase II (GCPII). Those containing carboxybenzyl or carboxyphenyl groups at the N-position exhibited potent inhibitory activity against GCPII. These indole-based compounds represent the first example of achiral GCPII inhibitors and demonstrate greater tolerance of the GCPII active site for ligands with significant structural difference from the endogenous substrate, N-acetyl-aspartylglutamate.

PMID:
21074428
DOI:
10.1016/j.bmcl.2010.10.109
[Indexed for MEDLINE]

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