4.5 Review

Strategies in the discovery of novel antifungal scaffolds

Journal

FUTURE MEDICINAL CHEMISTRY
Volume 8, Issue 12, Pages 1435-1454

Publisher

FUTURE SCI LTD
DOI: 10.4155/fmc-2016-0020

Keywords

antifungal drug resistance; antifungal lead compounds; drug repurposing; fungal biofilm inhibitors; invasive fungal infections; new antifungal scaffolds; strategies in antifungal drug discovery

Funding

  1. National Natural Science Foundation of China [81573283, 21502224]
  2. 863 Hi-Tech Program of China [2014AA020525]
  3. Science and Technology Commission of Shanghai [13431900301]
  4. Shanghai 'ShuGuang' Project [14SG33]
  5. Youth Foundation of Second Military Medical University [2014QN06]

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The development of next-generation antifungal agents with novel chemical scaffolds and new mechanisms of action is vital due to increased incidence and mortality of invasive fungal infections and severe drug resistance. This review will summarize current strategies to discover novel antifungal scaffolds. In particular, high-throughput screening, drug repurposing, antifungal natural products and new antifungal targets are focused on. New scaffolds with validated antifungal activity, their discovery and optimization process as well as structure-activity relationships are discussed in detail. Perspectives that could inspire future antifungal drug discovery are provided.

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