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Type: Journal article
Title: A hypoxia-activated antibacterial prodrug
Author: Yeoh, Y.Q.
Horsley, J.R.
Polyak, S.W.
Abell, A.D.
Citation: Bioorganic and Medicinal Chemistry Letters, 2020; 30(11):127140-1-127140-3
Publisher: Elsevier
Issue Date: 2020
ISSN: 0960-894X
Statement of
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.
RMID: 1000018578
DOI: 10.1016/j.bmcl.2020.127140
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Appears in Collections:Medicine publications

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