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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Detalhes bibliográficos
Publicado no:J Med Chem
Main Authors: 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.
Formato: Artigo
Idioma:Inglês
Publicado em: 2017
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Article
Acesso em linha: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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