Diverted Total Synthesis of the Baulamycins and Analogues Reveals an Alternate Mechanism of Action
Overview
Chemistry
Affiliations
The baulamycins were identified as in vitro siderophore biosynthesis inhibitors. Diverted total synthesis was used to construct the natural products and eight strategic analogues, three of which had improved inhibitory activity. Biological testing then revealed that membrane damage is the predominant mode of action in Staphylococcus aureus cells.
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Demeritte A, Wuest W Bioorg Med Chem. 2020; 28(23):115792.
PMID: 33038665 PMC: 7528826. DOI: 10.1016/j.bmc.2020.115792.
Stereoselective Synthesis of Baulamycin A.
Thielman J, Sherman D, Williams R J Org Chem. 2020; 85(5):3812-3823.
PMID: 31970985 PMC: 7271067. DOI: 10.1021/acs.joc.9b03443.
Dauner M, Skerra A Chembiochem. 2019; 21(5):601-606.
PMID: 31613035 PMC: 7079049. DOI: 10.1002/cbic.201900564.
Bailey D, Buckley B, Chernov M, Gulick A SLAS Discov. 2018; 23(10):1070-1082.
PMID: 29991301 PMC: 6246805. DOI: 10.1177/2472555218787140.