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Structural Optimization of Thiol-Based Inhibitors of Glutamate Carboxypeptidase II by Modification of the P1‘ Side Chain

✍ Scribed by Majer, Pavel; Hin, Bunda; Stoermer, Doris; Adams, Jessica; Xu, Weizheng; Duvall, Bridget R.; Delahanty, Greg; Liu, Qun; Stathis, Marigo J.; Wozniak, Krystyna M.; Slusher, Barbara S.; Tsukamoto, Takashi

Book ID
126330106
Publisher
American Chemical Society
Year
2006
Tongue
English
Weight
194 KB
Volume
49
Category
Article
ISSN
0022-2623

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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 compound