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

…, SA Shuler, BS Slusher, M Stathis, T Tsukamoto

文献索引：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 Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 24 p. 7222 - 7225

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被引用次数: 10

摘要

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 ...