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Extension of the polyanionic cosalane pharmacophore as a strategy for increasing anti-HIV potency

  1. Author:
    Cushman, M.
    Insaf, S.
    Paul, G.
    Ruell, J. A.
    De Clercq, E.
    Schols, D.
    Pannecouque, C.
    Witvrouw, M.
    Schaeffer, C. A.
    Turpin, J. A.
    Williamson, K.
    Rice, W. G.

  2. Author Address

    Cushman M Purdue Univ, Sch Pharm & Pharmacal Sci, Dept Med Chem & Mol Pharmacol W Lafayette, IN 47907 USA Purdue Univ, Sch Pharm & Pharmacal Sci, Dept Med Chem & Mol Pharmacol W Lafayette, IN 47907 USA Katholieke Univ Leuven, Rega Inst Med Res B-3000 Louvain Belgium NCI, Frederick Canc Res & Dev Ctr, Lab Antiviral Drug Mechanisms, SAIC Frederick Frederick, MD 21702 USA
    1. Year: 1999
  2. Journal: Journal of Medicinal Chemistry
    1. 42
    2. 10
    3. Pages: 1767-1777
  4. Type of Article: Article
  1. Abstract:

    The anti-HIV agent cosalane inhibits both the binding of gp120 to CD4 as well as an undefined postattachment event prior to reverse transcription. Several cosalane analogues having an extended polyanionic "pharmacophore" were designed based on a hypothetical model of the binding of cosalane to CD4. The analogues were synthesized, and a number of them displayed anti-HIV activity. One of the new analogues was found to possess enhanced potency as an anti-HIV agent relative to cosalane itself. Although the new analogues inhibited both HIV-1 and HTV-2, they were more potent as inhibitors of HIV-1 than HIV-2. Mechanism of action studies indicated that the most potent of the new analogues inhibited fusion of the viral envelope with the cell membrane at lower concentrations than it inhibited attachment, suggesting inhibition of fusion as the primary mechanism of action. [References: 29]

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