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Synthesis and Biological Evaluation of Thiol-Based Inhibitors of Glutamate Carboxypeptidase II: Discovery of an Orally Active GCP II Inhibitor

✍ Scribed by Majer, Pavel; Jackson, Paul F.; Delahanty, Greg; Grella, Brian S.; Ko, Yao-Sen; Li, Weixing; Liu, Qun; Maclin, Keith M.; Poláková, Jana; Shaffer, Kathryn A; Stoermer, Doris; Vitharana, Dilrukshi; Wang, Eric Yanjun; Zakrzewski, Anthony; Rojas, Camilo; Slusher, Barbara S.; Wozniak, Krystyna M.; Burak, Eric; Limsakun, Tharin; Tsukamoto, Takashi


Book ID
126399018
Publisher
American Chemical Society
Year
2003
Tongue
English
Weight
144 KB
Volume
46
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