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    Bioorg Med Chem. 2011 Aug 15;19(16):4895-902. doi: 10.1016/j.bmc.2011.06.061. Epub 2011 Jun 28.

    Oxadiazole derivatives containing 1,4-benzodioxan as potential immunosuppressive agents against RAW264.7 cells.

    Sun J, Cao N, Zhang XM, Yang YS, Zhang YB, Wang XM, Zhu HL.

    Source

    State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing 210093, PR China.

    Abstract

    A series of oxadiazole derivatives containing 1,4-benzodioxan (4a-4s) have been first synthesized for their potential immunosuppressive activity. Among the compounds, compound 4i showed the most potent biological activity against RAW264.7 cells (inhibition=37.66±2.34% for NO overproduction and IC(50)=0.05μM for iNOS). Docking simulation was performed to position compound 4i into the iNOS structure active site to determine the probable binding model. RT-PCR experiment results demonstrated that some of these compounds possessed good immunosuppressive activity against iNOS, especially for compound 4i. Therefore, compound 4i with potent inhibitory activity may be a potential agent.

    Crown Copyright © 2011. Published by Elsevier Ltd. All rights reserved.

    PMID:
    21782456
    [PubMed - indexed for MEDLINE]

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