A hypoxia-activated antibacterial prodrug.

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.

journal_name

Bioorg Med Chem Lett

authors

Yeoh YQ,Horsley JR,Polyak SW,Abell AD

doi

10.1016/j.bmcl.2020.127140

subject

Has Abstract

pub_date

2020-06-01 00:00:00

pages

127140

issue

11

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(20)30233-X

journal_volume

30

pub_type

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