A click chemistry approach to pleuromutilin derivatives. Part 3

extended footprinting analysis and excellent MRSA inhibition for a derivative with an adenine phenyl side chain

Publikation: Bidrag til tidsskriftTidsskriftartikelForskningpeer review

Resumé

Five promising pleuromutilin derivatives from our former studies, all containing adenine on various linkers, were supplemented with two new compounds. The binding to Escherichia coli ribosomes was verified by extensive chemical footprinting analysis. The ability to inhibit bacterial growth was investigated on two Staphylococcus aureus strains and compared to the pleuromutilin drugs tiamulin and valnemulin. Three of the compounds show an effect similar to tiamulin and one compound shows an excellent effect similar to valnemulin.

OriginalsprogEngelsk
TidsskriftBioorganic & Medicinal Chemistry Letters
Vol/bind24
Udgave nummer4
Sider (fra-til)1043-6
Antal sider4
ISSN0960-894X
DOI
StatusUdgivet - 15. feb. 2014

Fingeraftryk

Click Chemistry
Adenine
Derivatives
Escherichia coli
Growth
Chemical analysis
Pharmaceutical Preparations
tiamulin
valnemulin
pleuromutilin

Citer dette

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title = "A click chemistry approach to pleuromutilin derivatives. Part 3: extended footprinting analysis and excellent MRSA inhibition for a derivative with an adenine phenyl side chain",
abstract = "Five promising pleuromutilin derivatives from our former studies, all containing adenine on various linkers, were supplemented with two new compounds. The binding to Escherichia coli ribosomes was verified by extensive chemical footprinting analysis. The ability to inhibit bacterial growth was investigated on two Staphylococcus aureus strains and compared to the pleuromutilin drugs tiamulin and valnemulin. Three of the compounds show an effect similar to tiamulin and one compound shows an excellent effect similar to valnemulin.",
author = "Ida Dreier and Hansen, {Lykke H} and Poul Nielsen and Birte Vester",
note = "Copyright {\circledC} 2014 Elsevier Ltd. All rights reserved.",
year = "2014",
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T1 - A click chemistry approach to pleuromutilin derivatives. Part 3

T2 - extended footprinting analysis and excellent MRSA inhibition for a derivative with an adenine phenyl side chain

AU - Dreier, Ida

AU - Hansen, Lykke H

AU - Nielsen, Poul

AU - Vester, Birte

N1 - Copyright © 2014 Elsevier Ltd. All rights reserved.

PY - 2014/2/15

Y1 - 2014/2/15

N2 - Five promising pleuromutilin derivatives from our former studies, all containing adenine on various linkers, were supplemented with two new compounds. The binding to Escherichia coli ribosomes was verified by extensive chemical footprinting analysis. The ability to inhibit bacterial growth was investigated on two Staphylococcus aureus strains and compared to the pleuromutilin drugs tiamulin and valnemulin. Three of the compounds show an effect similar to tiamulin and one compound shows an excellent effect similar to valnemulin.

AB - Five promising pleuromutilin derivatives from our former studies, all containing adenine on various linkers, were supplemented with two new compounds. The binding to Escherichia coli ribosomes was verified by extensive chemical footprinting analysis. The ability to inhibit bacterial growth was investigated on two Staphylococcus aureus strains and compared to the pleuromutilin drugs tiamulin and valnemulin. Three of the compounds show an effect similar to tiamulin and one compound shows an excellent effect similar to valnemulin.

U2 - 10.1016/j.bmcl.2014.01.019

DO - 10.1016/j.bmcl.2014.01.019

M3 - Journal article

VL - 24

SP - 1043

EP - 1046

JO - Bioorganic & Medicinal Chemistry Letters

JF - Bioorganic & Medicinal Chemistry Letters

SN - 0960-894X

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