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  • Title: SAR studies of 4-acyl-1,6-dialkylpiperazin-2-one arenavirus cell entry inhibitors.
    Author: Plewe MB, Whitby LR, Naik S, Brown ER, Sokolova NV, Gantla VR, York J, Nunberg JH, Zhang L, Kalveram B, Freiberg AN, Boger DL, Henkel G, McCormack K.
    Journal: Bioorg Med Chem Lett; 2019 Nov 15; 29(22):126620. PubMed ID: 31537423.
    Abstract:
    Old World (Africa) and New World (South America) arenaviruses are associated with human hemorrhagic fevers. Efforts to develop small molecule therapeutics have yielded several chemical series including the 4-acyl-1,6-dialkylpiperazin-2-ones. Herein, we describe an extensive exploration of this chemotype. In initial Phase I studies, R1 and R4 scanning libraries were assayed to identify potent substituents against Old World (Lassa) virus. In subsequent Phase II studies, R6 substituents and iterative R1, R4 and R6 substituent combinations were evaluated to obtain compounds with improved Lassa and New World (Machupo, Junin, and Tacaribe) arenavirus inhibitory activity, in vitro human liver microsome metabolic stability and aqueous solubility.
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