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Issue 22, 2016
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Synthesis of amino heterocycle aspartyl protease inhibitors

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Aspartyl proteases are important pharmacological targets. Historically aspartyl proteases have been commonly targeted with transition state derived peptidomimetics. The strategy to develop aspartyl protease inhibitors has undertaken a dramatic paradigm shift in the last 10 years. The pharmaceutical industry in 2005 disclosed several scaffolds or “head groups” that prompted the field to move beyond peptidomimetic derived inhibitors. Since the discovery of the first amino heterocycle aspartyl protease inhibitor, the amino hydantoin, industry and academia have positioned themselves for a foothold on the new molecular space, designing a variety of related “head groups”. Both the design and synthetic efforts involved in constructing these scaffolds are varied and complex. Here we highlight the synthetic strategies used to access these amino heterocycle scaffolds.

Graphical abstract: Synthesis of amino heterocycle aspartyl protease inhibitors

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The article was received on 05 Mar 2016, accepted on 21 Apr 2016 and first published on 28 Apr 2016

Article type: Review Article
DOI: 10.1039/C5OB01842K
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Org. Biomol. Chem., 2016,14, 4970-4985

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    Synthesis of amino heterocycle aspartyl protease inhibitors

    R. K. Chambers, T. A. Khan, D. B. Olsen and B. E. Sleebs, Org. Biomol. Chem., 2016, 14, 4970
    DOI: 10.1039/C5OB01842K

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