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|Title:||A hypoxia-activated antibacterial prodrug|
|Citation:||Bioorganic and Medicinal Chemistry Letters, 2020; 30(11):127140-1-127140-3|
|Yuan Qi Yeoh, John R. Horsley, Steven W. Polyak, Andrew D. Abell|
|Abstract:||A prodrug based on a known antibacterial compound is reported to target Staphylococcus aureus and Escherichia coli under reductive conditions. The prodrug was prepared by masking the N-terminus and side chain amines of a component lysine residue as 4-nitrobenzyl carbamates. Activation to liberate the antibacterial was demonstrated on treatment with a model reductant, tin(II) chloride. The bioactivity of 1 was confirmed in antibacterial susceptibility assays whereas prodrug 2 was inactive.|
|Keywords:||Antibacterial; E. coli; Hypoxia-activated; Prodrug; S. aureus|
|Rights:||© 2020 Elsevier Ltd. All rights reserved.|
|Appears in Collections:||Medicine publications|
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