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Synthesis of Azaspirocycles and their Evaluation in Drug Discovery


  • We thank F. Hoffmann–La Roche AG for support of this research. J.A.B. is grateful to Novartis and the Roche Research Foundation for graduate fellowship support. This research was supported by a grant from ETH-Z (0-20449-07). Dr. Sven Hobbie (University of Zurich) is acknowledged for measuring the MIC values.


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Make it spiro! Readily synthesized heteroatom-substituted spiro[3.3]heptanes generally show higher aqueous solubility than their cyclohexane analogues, and show a trend towards higher metabolic stability. The novel framework can be mounted onto scaffolds of druglike structures, such as fluoroquinolones, to afford active compounds with similar or even improved metabolic stability.