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  • Title: Discovery and Synthesis of Heterocyclic Carboxamide Derivatives as Potent Anti-norovirus Agents.
    Author: Ohba M, Oka T, Ando T, Arahata S, Ikegaya A, Takagi H, Ogo N, Owada K, Kawamori F, Wang Q, Saif LJ, Asai A.
    Journal: Chem Pharm Bull (Tokyo); 2016; 64(5):465-75. PubMed ID: 27150478.
    Abstract:
    There is an urgent need for structurally novel anti-norovirus agents. In this study, we describe the synthesis, anti-norovirus activity, and structure-activity relationship (SAR) of a series of heterocyclic carboxamide derivatives. Heterocyclic carboxamide 1 (50% effective concentration (EC50)=37 µM) was identified by our screening campaign using the cytopathic effect reduction assay. Initial SAR studies suggested the importance of halogen substituents on the heterocyclic scaffold and identified 3,5-di-boromo-thiophene derivative 2j (EC50=24 µM) and 4,6-di-fluoro-benzothiazole derivative 3j (EC50=5.6 µM) as more potent inhibitors than 1. Moreover, their hybrid compound, 3,5-di-bromo-thiophen-4,6-di-fluoro-benzothiazole 4b, showed the most potent anti-norovirus activity with a EC50 value of 0.53 µM (70-fold more potent than 1). Further investigation suggested that 4b might inhibit intracellular viral replication or the late stage of viral infection.
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