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Issue 22, 2012
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Applications of 3-aminolactams: design, synthesis, and biological evaluation of a library of potential dimerisation inhibitors of HIV1-protease

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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 (EC50). 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.

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

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Publication details

The article was received on 09 Feb 2012, accepted on 05 Apr 2012 and first published on 05 Apr 2012


Article type: Paper
DOI: 10.1039/C2OB25291K
Citation: Org. Biomol. Chem., 2012,10, 4348-4354
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    Applications of 3-aminolactams: design, synthesis, and biological evaluation of a library of potential dimerisation inhibitors of HIV1-protease

    E. Pinyol, S. Frutos, D. Grillo-Bosch, E. Giralt, B. Clotet, J. A. Esté and A. Diez, Org. Biomol. Chem., 2012, 10, 4348
    DOI: 10.1039/C2OB25291K

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