560131-50-2Relevant academic research and scientific papers
The discovery and structure-activity relationships of indole-based inhibitors of glutamate carboxypeptidase II
Grella, Brian,Adams, Jessica,Berry, James F.,Delahanty, Greg,Ferraris, Dana V.,Majer, Pavel,Ni, Chiyou,Shukla, Krupa,Shuler, Scott A.,Slusher, Barbara S.,Stathis, Marigo,Tsukamoto, Takashi
scheme or table, p. 7222 - 7225 (2011/01/03)
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.
