3 research outputs found

    Enantioselective Biomimetic Total Syntheses of Katsumadain and Katsumadain C

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    Enantioselective total syntheses of katsumadain and katsumadain C were achieved concisely through a biomimetic approach. Assembly of styryl-2-pyranone (<b>3</b>) and monoterpene <b>6</b> via acid-promoted regio- and stereoselective C–C bond formation afforded katsumadain (<b>2</b>), which underwent the photoinduced [2 + 2] dimerization in a head-to-tail mode to furnish katsumadain C (<b>1</b>)

    Chlorine Dioxide Inactivation of Enterovirus 71 in Water and Its Impact on Genomic Targets

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    To control the waterborne transmission of enterovirus 71­(EV71), which is associated with hand foot and mouth disease (HFMD), it is essential to know the inactivation effectiveness of disinfectants on EV71 in water. In this article, we present a comparative analysis of the effects on EV71 following exposure to chlorine dioxide (ClO<sub>2</sub>) under different doses, pH, and temperature conditions. We show that the EV71 exhibited strong resistance to ClO<sub>2</sub> (more than the MS2 standard) and that <i>C<sub>t</sub></i> value ranges required for a 4-log reduction of EV71 in buffered, disinfectant demand-free water at pH 7.2 and 20 °C by ClO<sub>2</sub> were 4.24–6.62 mg/L·min according to the efficiency factor Hom model. ClO<sub>2</sub> inactivation of the virus was temperature- and pH-dependent. The virucidal efficiency was higher at pH 8.2 than at pH 5.6 and pH 7.2 and higher at 36 °C than at 4 and 20 °C. In addition, we also observed the impact of ClO<sub>2</sub> on the entire viral genome using RT-PCR, which indicated that the 5′ noncoding region (5′-NCR) within the EV71 genome, specifically the 1–118 nt region, was the most easily damaged by ClO<sub>2</sub> and correlated with viral infectivity. Our study has not only provided guidelines for EV71 disinfection strategies of waste and drinking water, but also confirmed the importance of the 5′-NCR for EV71 infectivity and may demonstrate a general inactivation by ClO<sub>2</sub> of enteric virus by damaging the 5′-NCR. Furthermore, 5′-NCR can be used as a target region for PCR to investigate infectious virus contamination in environmental water and evaluate the inactivation effects of ClO<sub>2</sub>

    Discovery of Imidazo[1,2-α][1,8]naphthyridine Derivatives as Potential HCV Entry Inhibitor

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    RO8191 represents a newly discovered small-molecule IFN-like agent that displays potent anti-HCV activity. With it as lead, a series of compounds bearing an imidazo­[1,2-α]­[1,8]­naphthyridine core and an amide bond-linked side chain were designed and synthesized. These compounds were evaluated on HCV cell culture system (HCVcc-hRluc-JFH1), and some of them exhibited remarkable anti-HCV activity (EC<sub>50</sub> = 0.017–0.159 μM) and low toxicity (CC<sub>50</sub> > 25 μM). Moreover, it was revealed that these newly identified anti-HCV agents exert their antiviral effect through a distinct mechanism of action from that of RO8191 by targeting the viral entry process. Thus, our study provides a starting point for the development of potential HCV entry inhibitor
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