4.6 Article

Flustramine inspired synthesis and biological evaluation of pyrroloindoline triazole amides as novel inhibitors of bacterial biofilms

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ORGANIC & BIOMOLECULAR CHEMISTRY
卷 9, 期 15, 页码 5476-5481

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ROYAL SOC CHEMISTRY
DOI: 10.1039/c1ob05605k

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  1. National Institute of Health [GM055769]
  2. NATIONAL INSTITUTE OF GENERAL MEDICAL SCIENCES [R01GM055769] Funding Source: NIH RePORTER

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Anti-biofilm agents have been developed based upon the flustramine family of alkaloids isolated from Flustra foliacea. A Garg interrupted Fischer indolization reaction was employed to access a core pyrroloindoline scaffold that was subsequently employed to create a pyrroloindoline triazole amide library. Screening for the ability to modulate biofilm formation against strains of Gram-positive and Gram-negative bacteria identified several compounds with low micromolar, non-toxic IC50 values.

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