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                <text>Coronavirus</text>
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                <text>Dominio científico: Coronavirus</text>
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              <text>Design, Synthesis and Investigation of the Potential Anti-Inflammatory Activity of 7-&lt;i&gt;O&lt;/i&gt;-Amide Hesperetin Derivatives</text>
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              <text>Yilong Zhang, Yan Zheng, Wen Shi, Yahui Guo, Tao Xu, Zeng Li, Cheng Huang, Jun Li</text>
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              <text>To develop new anti-inflammatory agents, a series of 7-O-amide hesperetin derivatives was designed, synthesized and evaluated for anti-inflammatory activity using RAW264.7 cells. All compounds showed inhibitory effect on LPS-induced NO production. Among them, 7-O-(2-(Propylamino)-2-oxoethyl)hesperetin (4d) and 7-O-(2-(Cyclopentylamino)-2-oxoethyl)hesperetin (4k) with hydrophobic side chains exhibited the most potent NO inhibitory activity (IC50 = 19.32 and 16.63 &amp;#956;M, respectively), showing stronger inhibitory effect on the production of pro- inflammatory cytokines tumor necrosis factor (TNF-&amp;#945;), interleukin-6 (IL-6) and interleukin-1&amp;#946; (IL-1&amp;#946;) than indomethacin and celecoxib at 10 &amp;#956;M. The structure-activity relationships (SARs) suggested that the 7-O-amide unit was buried in a medium-sized hydrophobic cavity of the bound receptor. Furthermore, compound 4d could also significantly suppress the expression of inducible nitric oxide synthase enzymes (iNOS) and cyclooxygenase-2 (COX-2), through the nuclear factor-kappa B (NF-&amp;#954;B) signaling pathway.</text>
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              <text>2019</text>
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              <text>hesperetin derivatives, Synthesis, Inflammatory, NF-κB, structure-activity relationships</text>
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              <text>DOI: 10.3390/molecules24203663</text>
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          <name>Source</name>
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              <text>Molecules</text>
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          <name>Publisher</name>
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              <text>MDPI AG</text>
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          <name>Coverage</name>
          <description>The spatial or temporal topic of the resource, the spatial applicability of the resource, or the jurisdiction under which the resource is relevant</description>
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              <text>Organic chemistry</text>
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              <text>EN</text>
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