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

A series of thiol-based glutamate carboxypeptidase II (GCPII) inhibitors have been synthesized with either a 3-(mercaptomethyl)benzoic acid or 2-(2-mercaptoethyl)benzoic acid scaffold. Potent inhibitors were identified from each of the two scaffolds with IC50 values in the single-digit nanomolar ran...

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Veröffentlicht in:	Journal of medicinal chemistry 2012-06, Vol.55 (12), p.5922-5932
Hauptverfasser:	Stoermer, Doris, Vitharana, Dilrukshi, Hin, Niyada, Delahanty, Greg, Duvall, Bridget, Ferraris, Dana V, Grella, Brian S, Hoover, Randall, Rojas, Camilo, Shanholtz, Megan K, Smith, Kyle P, Stathis, Marigo, Wu, Ying, Wozniak, Krystyna M, Slusher, Barbara S, Tsukamoto, Takashi
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Benzoates - chemical synthesis Benzoates - pharmacokinetics Benzoates - pharmacology Benzoates - therapeutic use Chemistry Techniques, Synthetic Drug Design Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - pharmacokinetics Enzyme Inhibitors - pharmacology Enzyme Inhibitors - therapeutic use Glutamate Carboxypeptidase II - antagonists & inhibitors Humans Inhibitory Concentration 50 Neuralgia - drug therapy Rats
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