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Published in

Beilstein-Institut, Beilstein Journal of Organic Chemistry, (15), p. 1468-1474, 2019

DOI: 10.3762/bjoc.15.147

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Synthesis and biological evaluation of truncated derivatives of abyssomicin C as antibacterial agents

This paper is made freely available by the publisher.
This paper is made freely available by the publisher.

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Abstract

The synthesis and antibacterial activity of two new highly truncated derivatives of the natural product abyssomicin C are reported. This work outlines the limits of structural truncation of the natural product and consequently provides insights for further structure–activity relationship studies towards novel antibiotics targeting 4-amino-4-deoxychorismate (ADC) synthase. Specifically, it is demonstrated that the synthetically challenging bicyclic motif is essential for activity towards methicillin-resistant Staphylococcus aureus (MRSA).