Discovery of a para-Acetoxy-benzyl Ester Prodrug of a Hydroxamate-Based Glutamate Carboxypeptidase II Inhibitor as Oral Therapy for Neuropathic Pain

4-Carboxy-α-[3-(hydroxyamino)-3-oxopropyl]-benzenepropanoic acid 1 is a potent hydroxamate-based inhibitor of glutamate carboxypeptidase II. In an attempt to improve its poor oral pharmacokinetics, we synthesized a series of prodrugs by masking its hydrophilic hydroxamate group. Prodrugs were evalua...

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Bibliografische gegevens
Gepubliceerd in:J Med Chem
Hoofdauteurs: Rais, Rana, Vávra, Jan, Tichý, Tomáš, Dash, Ranjeet P., Gadiano, Alexandra J., Tenora, Lukáš, Monincová, Lenka, Bařinka, Cyril, Alt, Jesse, Zimmermann, Sarah C., Slusher, C. Ethan, Wu, Ying, Wozniak, Krystyna, Majer, Pavel, Tsukamoto, Takashi, Slusher, Barbara S.
Formaat: Artigo
Taal:Inglês
Gepubliceerd in: 2017
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Article
Online toegang:https://ncbi.nlm.nih.gov/pmc/articles/PMC5795597/
https://ncbi.nlm.nih.gov/pubmed/28759215
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.7b00825
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