Synthesis and Biological Evaluation of the Antimicrobial Natural Product Lipoxazolidinone A
Open Access
- 10 June 2018
- journal article
- research article
- Published by Wiley in Angewandte Chemie International Edition
- Vol. 57 (28) , 8682-8686
Abstract
Natural products have historically been a major source of antibiotics and therefore novel scaffolds are constantly of interest. 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 analogues 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.Keywords
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Funding Information
- National Institute of General Medical Sciences (1R01GM110154)
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