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  • Title: Discovery of a small molecule inhibitor through interference with the gp120-CD4 interaction.
    Author: Williams DH, Adam F, Fenwick DR, Fok-Seang J, Gardner I, Hay D, Jaiessh R, Middleton DS, Mowbray CE, Parkinson T, Perros M, Pickford C, Platts M, Randall A, Siddle D, Stephenson PT, Tran TD, Vuong H.
    Journal: Bioorg Med Chem Lett; 2009 Sep 01; 19(17):5246-9. PubMed ID: 19620004.
    Abstract:
    A series of piperazine derivatives were designed and synthesised as gp120-CD4 inhibitors. SAR studies led to the discovery of potent inhibitors in a cell based anti viral assay represented by compounds 9 and 28. The rat pharmacokinetic and antiviral profiles of selected compounds are also presented.
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