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Bioorg Med Chem. 2013 Sep 15;21(18):5876-85. doi: 10.1016/j.bmc.2013.07.004. Epub 2013 Jul 12.

Investigation of acyclic uridine amide and 5'-amido nucleoside analogues as potential inhibitors of the Plasmodium falciparum dUTPase.

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  • 1Division of Biological Chemistry and Drug Discovery, College of Life Science, University of Dundee, Sir James Black Centre, UK.


Previously we have shown that trityl and diphenyl deoxyuridine derivatives and their acyclic analogues can inhibit Plasmodium falciparum dUTPase (PfdUTPase). We report the synthesis of conformationally restrained amide derivatives as inhibitors PfdUTPase, including both acyclic and cyclic examples. Activity was dependent on the orientation and location of the amide constraining group. In the case of the acyclic series, we were able to obtain amide-constrained analogues which showed similar or greater potency than the unconstrained analogues. Unfortunately these compounds showed lower selectivity in cellular assays.

Copyright © 2013 The Authors. Published by Elsevier Ltd.. All rights reserved.

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