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- W2998777768 abstract "Decaprenylphosphoryl-β-d-ribose 2'-epimerase (DprE1) is an essential enzyme in Mycobacterium tuberculosis and has recently been studied as a potential drug target, with inhibitors progressing to clinical studies. Here we describe the identification of a novel series of morpholino-pyrimidine DprE1 inhibitors. These were derived from a phenotypic high-throughput screening (HTS) hit with suboptimal physicochemical properties. Optimization strategies included scaffold-hopping, synthesis, and evaluation of fragments of the lead compounds and property-focused optimization. The resulting optimized compounds had much improved physicochemical properties and maintained enzyme and cellular potency. These molecules demonstrated potent efficacy in an in vivo tuberculosis murine infection model." @default.
- W2998777768 created "2020-01-23" @default.
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- W2998777768 date "2020-01-10" @default.
- W2998777768 modified "2023-10-18" @default.
- W2998777768 title "<i>Mycobacterium tuberculosis</i> Decaprenylphosphoryl-β-<scp>d</scp>-ribose Oxidase Inhibitors: Expeditious Reconstruction of Suboptimal Hits into a Series with Potent in Vivo Activity" @default.
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- W2998777768 doi "https://doi.org/10.1021/acs.jmedchem.9b01561" @default.
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