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• W2057789922 startingPage "6209" @default.
• W2057789922 abstract "Hypoxanthine–guanine–(xanthine) phosphoribosyltransferase (HG(X)PRT) is crucial for the survival of malarial parasites Plasmodium falciparum (Pf) and Plasmodium vivax (Pv). Acyclic nucleoside phosphonates (ANPs) are inhibitors of HG(X)PRT and arrest the growth of Pf in cell culture. Here, a novel class of ANPs containing trisubstituted nitrogen (aza-ANPs) has been synthesized. These compounds have a wide range of Ki values and selectivity for human HGPRT, PfHGXPRT, and PvHGPRT. The most selective and potent inhibitor of PfHGXPRT is 9-[N-(3-methoxy-3-oxopropyl)-N-(2-phosphonoethyl)-2-aminoethyl]hypoxanthine (Ki = 100 nM): no inhibition could be detected against the human enzyme. This compound exhibits the highest ever reported selectivity for PfHGXPRT compared to human HGPRT. For PvHGPRT, 9-[N-(2-carboxyethyl)-N-(2-phosphonoethyl)-2-aminoethyl]guanine has a Ki of 50 nM, the best inhibitor discovered for this enzyme to date. Docking of these compounds into the known structures of human HGPRT in complex with ANP-based inhibitors suggests reasons for the variations in affinity, providing insights for the design of antimalarial drug candidates." @default.
• W2057789922 created "2016-06-24" @default.
• W2057789922 creator A5026188443 @default.
• W2057789922 creator A5045317036 @default.
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• W2057789922 date "2012-06-22" @default.
• W2057789922 modified "2023-09-30" @default.
• W2057789922 title "Synthesis of Novel <i>N</i>-Branched Acyclic Nucleoside Phosphonates As Potent and Selective Inhibitors of Human, Plasmodium falciparum and Plasmodium vivax 6-Oxopurine Phosphoribosyltransferases" @default.
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• W2057789922 doi "https://doi.org/10.1021/jm300662d" @default.
• W2057789922 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/22725979" @default.
• W2057789922 hasPublicationYear "2012" @default.
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