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

Beilstein Journal of Organic Chemistry

Maja Genheden¹  D. G. Joakim Larsson¹  Carlo Cassani²  Peter Fodran²  Carl-Johan Wallentin²  Johanna Kollback²  Thomas Olsson²  Leticia Monjas² 

[1] Centre for Antibiotic Resistance Research (CARe), University of Gothenburg, Gothenburg, Sweden;Department of Chemistry and Molecular Biology, University of Gothenburg, Kemigården 4, 412 96, Gothenburg, Sweden;

关键词: abyssomicin C;    antibiotic;    antibiotic resistance;    MRSA;    truncated natural products;   

DOI  :  10.3762/bjoc.15.147

来源: DOAJ

【 摘 要 】

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).

【 授权许可】

Unknown