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Synthesis and Biological Evaluation of the Antimicrobial Natural Product Lipoxazolidinone A

preprint
submitted on 05.04.2018, 18:19 and posted on 09.04.2018, 16:09 by Jonathan J. Mills, Kaylib R. Robinson, Troy E. Zehnder, Joshua G. Pierce
The lipoxazolidinone family of marine natural products, with an unusual 4-oxazolidinone heterocycle at their core, represents a new scaffold for antimicrobial discovery; however, questions regarding their mechanism of action and high lipophilicity have likely slowed follow-up studies. Herein, we report the first synthesis of lipoxazolidinone A, 15 structural analogs to explore its active pharmacophore, and initial resistance and mechanism of action studies. These results suggest that 4-oxazolidinones are valuable scaffolds for antimicrobial development and reveal simplified lead compounds for further optimization.

Funding

NIH (1R01GM110154)

History

Email Address of Submitting Author

jgpierce@ncsu.edu

Institution

NC State University

Country

United States

ORCID For Submitting Author

0000-0001-9194-3765

Declaration of Conflict of Interest

No Conflict of Interest

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