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Synthesis and Properties of a New Water-Soluble Prodrug of the Adenosine A2A Receptor Antagonist MSX-2

Pharma-Center Bonn, Pharmaceutical Institute, Pharmaceutical Chemistry I, An der Immenburg 4, D-53121 Bonn, Germany
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Molecules 2008, 13(2), 348-359; https://doi.org/10.3390/molecules13020348
Received: 29 January 2008 / Revised: 11 February 2008 / Accepted: 11 February 2008 / Published: 12 February 2008
(This article belongs to the Special Issue Prodrugs)
The compound L-valine-3-{8-[(E)-2-[3-methoxyphenyl)ethenyl]-7-methyl-1-propargylxanthine-3-yl}propyl ester hydrochloride (MSX-4) was synthesized as an aminoacid ester prodrug of the adenosine A2A receptor antagonist MSX-2. It was found to bestable in artificial gastric acid, but readily cleaved by pig liver esterase. View Full-Text
Keywords: Prodrug; adenosine receptor antagonist; MSX-4; water-solubility; Parkinson’s disease; esterase. Prodrug; adenosine receptor antagonist; MSX-4; water-solubility; Parkinson’s disease; esterase.
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Vollmann, K.; Qurishi, R.; Hockemeyer, J.; Müller, C.E. Synthesis and Properties of a New Water-Soluble Prodrug of the Adenosine A2A Receptor Antagonist MSX-2. Molecules 2008, 13, 348-359.

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