Applications of 3-aminolactams: design, synthesis, and biological evaluation of a library of potential dimerisation inhibitors of HIV1-protease

Applications of 3-aminolactams: design, synthesis, and biological evaluation of a library of potential dimerisation inhibitors of HIV1-protease

Online publication: 05/04/2013

Abstract:

In the context of our studies on the applications of 3-aminolactams as conformationally restricted pseudodipeptides, we report here the synthesis of a library of potential dimerisation inhibitors of HIV1-protease. Two of the pseudopeptides were active on the wild type virus (HIV1) at micromolar levels (EC(50)). Although the peptides showed lower anti-viral activity than previously reported dimerisation inhibitors, our results demonstrate that the piperidone moiety does not prevent cell penetration, and hence that such derivatization is compatible with potential anti-HIV treatment. Read abstract online in Organic & Biomolecular Chemistry

Authors: Eulàlia Pinyol1,  Silvia Frutos1,  Dolors Grillo-Bosch1,  Ernest Giralt1,2,  Bonaventura Clotet3,  Jose A. Esté3 and Anna Diez1,4 1Institute for Research in Biomedicine, Barcelona Science Park, 2Departament de Química Orgànica, Facultat de Química, Universitat de Barcelona 3Fundació IrsiCaixa, Hospital Universitari Trias i Pujol, Badalona, Spain 4Laboratori de Química Orgànica, Facultat de Farmàcia, Universitat de Barcelona
  • Doi Code: Org Biomol Chem. 2012 Jun 14;10(22):4348-54. doi: 10.1039/c2ob25291k. Epub 2012 Apr 30

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