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Antiretroviral drug
BIT225
Другие языки:

    BIT225

    Подписчиков: 0, рейтинг: 0
    BIT225
    BIT225.svg
    Names
    IUPAC name
    N-Carbamimidoyl-5-(1-methyl-1H-pyrazol-4-yl)-2-naphthamide
    Other names
    BIT-225
    Identifiers
    3D model (JSmol)
    ChemSpider
    PubChem CID
    UNII
    • InChI=1S/C16H15N5O/c1-21-9-12(8-19-21)13-4-2-3-10-7-11(5-6-14(10)13)15(22)20-16(17)18/h2-9H,1H3,(H4,17,18,20,22)
      Key: WVROWPPEIMRGAB-UHFFFAOYSA-N
    • InChI=1/C16H15N5O/c1-21-9-12(8-19-21)13-4-2-3-10-7-11(5-6-14(10)13)15(22)20-16(17)18/h2-9H,1H3,(H4,17,18,20,22)
      Key: WVROWPPEIMRGAB-UHFFFAOYAP
    • CN1C=C(C=N1)C2=CC=CC3=C2C=CC(=C3)C(=O)NC(=N)N
    Properties
    C16H15N5O
    Molar mass 293.330 g·mol−1
    Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).

    BIT225 is an experimental drug candidate under development by Biotron Limited for use in the treatment of both HIV and hepatitis C infection. By blocking Vpu ion channel activity, it disrupts HIV assembly within host monocyte cells; its method of action is a first for HIV drugs. Because it targets replication in monocyte derived macrophages, it offers promise for treatment of viral reservoirs that are unaffected by standard treatments. The activity of BIT225 is post-virus integration, with no direct effects on the HIV enzymes reverse transcriptase and protease. Since Vpu ion channel activity is highly conserved, the virus is unlikely to become resistant via generation of Vpu ion-independent virus. In addition, the drug also has been credited with curing hepatitis C after 12 weeks of treatment.


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