✦ LIBER ✦

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

✍ Scribed by Brian Grella; Jessica Adams; James F. Berry; Greg Delahanty; Dana V. Ferraris; Pavel Majer; Chiyou Ni; Krupa Shukla; Scott A. Shuler; Barbara S. Slusher; Marigo Stathis; Takashi Tsukamoto

Book ID: 104005059
Publisher: Elsevier Science
Year: 2010
Tongue: English
Weight: 687 KB
Volume: 20
Category: Article
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2010.10.109

No coin nor oath required. For personal study only.

✦ Synopsis

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.

📜 SIMILAR VOLUMES

Structure-Activity Relationships of Glut

Structure-Activity Relationships of Glutamate Carboxypeptidase II (GCPII) Inhibitors

✍ V. Ferraris, D.; Shukla, K.; Tsukamoto, T. 📂 Article 📅 2012 🏛 Bentham Science Publishers 🌐 English ⚖ 796 KB

Discovery and Structure−Activity Relatio

Discovery and Structure−Activity Relationships of Novel Piperidine Inhibitors of Farnesyltransferase

✍ Nara, Shinji; Tanaka, Rieko; Eishima, Jun; Hara, Mitsunobu; Takahashi, Yuichi; O 📂 Article 📅 2003 🏛 American Chemical Society 🌐 English ⚖ 129 KB

Synthesis and Biological Evaluation of H

Synthesis and Biological Evaluation of Hydroxamate-Based Inhibitors [cf. (IX)] of Glutamate Carboxypeptidase II.

✍ Doris Stoermer; Qun Liu; Monicia R. Hall; Juliet M. Flanary; Ajit G. Thomas; Cam 📂 Article 📅 2003 🏛 John Wiley and Sons ⚖ 131 KB

Discovery and Structure−Activity Relatio

Discovery and Structure−Activity Relationships of Imidazole-Containing Tetrahydrobenzodiazepine Inhibitors of Farnesyltransferase

✍ Ding, Charles Z.; Batorsky, Roberta; Bhide, Rajeev; Chao, Hannguang J.; Cho, You 📂 Article 📅 1999 🏛 American Chemical Society 🌐 English ⚖ 159 KB

Synthesis of Urea-Based Inhibitors as Ac

Synthesis of Urea-Based Inhibitors as Active Site Probes of Glutamate Carboxypeptidase II: Efficacy as Analgesic Agents

✍ Kozikowski, Alan P.; Zhang, Jiazhong; Nan, Fajun; Petukhov, Pavel A.; Grajkowska 📂 Article 📅 2004 🏛 American Chemical Society 🌐 English ⚖ 197 KB

Design, Synthesis, and Pharmacological E

Design, Synthesis, and Pharmacological Evaluation of Glutamate Carboxypeptidase II (GCPII) Inhibitors Based on Thioalkylbenzoic Acid Scaffolds

✍ Stoermer, Doris; Vitharana, Dilrukshi; Hin, Niyada; Delahanty, Greg; Duvall, Bri 📂 Article 📅 2012 🏛 American Chemical Society 🌐 English ⚖ 704 KB