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N2′‐Branched Acyclic Nucleoside Phosphonates Containing 9‐Deazahypoxanthine as Inhibitors of Plasmodium falciparum 6‐Oxopurine Phosphoribosyltransferase by Karolína Vaňková; Dianne T. Keough; Dana Hocková; Luke W. Guddat; Zlatko Janeba is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

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## Abstract Twelve N2′‐branched acyclic nucleoside phosphonates and bisphosphonates were synthesized as potential inhibitors of Plasmodium falciparum hypoxanthine‐guanine‐xanthine phosphoribosyltransferase (PfHGXPRT), the key enzyme in the purine salvage pathway for production of purine nucleotides. The chemical structures were designed with the aim to study selectivity of the inhibitors for PfHGXPRT over human HGPRT. The newly prepared compounds contain 9‐deazahypoxanthine connected to a phosphonate group via a five‐atom‐linker bearing a nitrogen atom (N2′) as a branching point. All compounds, with the additional phosphonate group(s) in the second aliphatic linker attached to N2′ atom, were low micromolar inhibitors of PfHGXPRT with low to modest selectivity for the parasite enzyme over human HGPRT. The effect of the addition of different chemical groups/linkers to N2′ atom on the inhibition constants and selectivity is discussed.

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Author

Karolína Vaňková; Dianne T. Keough; Dana Hocková; Luke W. Guddat; Zlatko Janeba

Publisher

Wiley

Published

2023

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)