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  • Title: Design, synthesis, and antiviral evaluation of purine-β-lactam and purine-aminopropanol hybrids.
    Author: D'hooghe M, Mollet K, De Vreese R, Jonckers TH, Dams G, De Kimpe N.
    Journal: J Med Chem; 2012 Jun 14; 55(11):5637-41. PubMed ID: 22519297.
    Abstract:
    Purine-β-lactam chimera were prepared as a novel class of hybrid systems through N-alkylation of 6-benzylamino- or 6-benzyloxypurine with (ω-haloalkyl)-β-lactams, followed by reductive ring opening of the β-lactam ring by LiEt(3)BH to provide an entry into the class of purine-aminopropanol hybrids. Both new types of hybrid systems were assessed for their antiviral activity and cytotoxicity, resulting in the identification of eight purine-β-lactam hybrids and two purine-aminopropanol hybrids as promising lead structures.
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