A hypoxia-activated antibacterial prodrug.

Yeoh, Yuan Qi; Horsley, John R; Polyak, Steven W; Abell, Andrew D

Yeoh, Yuan Qi; Horsley, John R; Polyak, Steven W; Abell, Andrew D.

Afiliación

Yeoh YQ; ARC Centre of Excellence for Nanoscale BioPhotonics (CNBP), Department of Chemistry, The University of Adelaide, North Terrace, Adelaide, SA 5005, Australia.
Horsley JR; ARC Centre of Excellence for Nanoscale BioPhotonics (CNBP), Department of Chemistry, The University of Adelaide, North Terrace, Adelaide, SA 5005, Australia.
Polyak SW; School of Biological Sciences, Department of Molecular and Cellular Biology, The University of Adelaide, North Terrace, Adelaide, SA 5005, Australia. Electronic address: Steven.Polyak@unisa.edu.au.
Abell AD; ARC Centre of Excellence for Nanoscale BioPhotonics (CNBP), Department of Chemistry, The University of Adelaide, North Terrace, Adelaide, SA 5005, Australia. Electronic address: andrew.abell@adelaide.edu.au.

Bioorg Med Chem Lett ; 30(11): 127140, 2020 06 01.

Article en En | MEDLINE | ID: mdl-32247730

ABSTRACT

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.

Asunto(s)

Antibacterianos/química; Profármacos/química; Antibacterianos/síntesis química; Antibacterianos/farmacología; Escherichia coli/efectos de los fármacos; Pruebas de Sensibilidad Microbiana; Profármacos/síntesis química; Profármacos/farmacología; Staphylococcus aureus/efectos de los fármacos; Compuestos de Estaño/farmacología

Palabras clave

Antibacterial; E. coli; Hypoxia-activated; Prodrug; S. aureus

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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Profármacos / Antibacterianos Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2020 Tipo del documento: Article País de afiliación: Australia Pais de publicación: ENGLAND / ESCOCIA / GB / GREAT BRITAIN / INGLATERRA / REINO UNIDO / SCOTLAND / UK / UNITED KINGDOM

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