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Next-generation heterocyclic electrophiles as small-molecule covalent MurA inhibitors [Elektronski vir]Ábrányi-Balogh, Péter ...Heterocyclic electrophiles as small covalent fragments showed promising inhibitory activity on the antibacterial target MurA (UDP-N-acetylglucosamine 1-carboxyvinyltransferase, EC:2.5.1.7). Here, we ... report the second generation of heterocyclic electrophiles: the quaternized analogue of the heterocyclic covalent fragment library with improved reactivity and MurA inhibitory potency. Quantum chemical reaction barrier calculations, GSH (L-glutathione) reactivity assay, and thrombin counter screen were also used to demonstrate and explain the improved reactivity and selectivity of the N-methylated heterocycles and to compare the two generations of heterocyclic electrophiles.Source: Pharmaceuticals [Elektronski vir]. - ISSN 1424-8247 (Vol. 15, iss. 12, art. 1484, 2022, 10 str.)Type of material - e-article ; adult, seriousPublish date - 2022Language - englishCOBISS.SI-ID - 132462339
Author
Ábrányi-Balogh, Péter |
Keeley, Aaron |
Ferenczy, György G. |
Petri, László |
Imre, Tímea |
Grabrijan, Katarina |
Hrast, Martina |
Knez, Damijan, farmacevt |
Ilaš, Janez |
Gobec, Stanislav, 1970- |
Keserü M., György
Topics
Farmacevtska kemija |
Bakterijska rezistenca |
kovalentni inhibitor |
heterociklični elektrofili |
označevanje cisteina |
kvaternizacija |
MurA |
covalent inhibitor |
heterocyclic electrophiles |
cysteine labelling |
quaternization |
MurA
Author | Ábrányi-Balogh, Péter ... |
Title | Next-generation heterocyclic electrophiles as small-molecule covalent MurA inhibitors [Elektronski vir] |
Publication date | 2022-11-29 |
COBISS.SI-ID | 132462339 |
Publication version in repository | Publisher's version |
Publication licence | Creative Commons Attribution 4.0 International |
Embargo | Immediate publication for public |
Project(s) from which the publication was funded
Title | Acronym | Project ID | Funder |
---|---|---|---|
Kovalentni pristop k boju proti bakterijski rezistenci | N1-0169-2021 |
Javna agencija za znanstvenoraziskovalno in inovacijsko dejavnost Republike Slovenije |
|
Razvoj protibakteriskih učinkovin z delovanjem na validirane tarče v biosintezi peptidoglikana | J1-2484-2020 |
Javna agencija za znanstvenoraziskovalno in inovacijsko dejavnost Republike Slovenije |
|
FRAGments training NETwork | FRAGNET | 675899 |
European Commission |
Files that belong to the publication
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https://www.mdpi.com/1424-8247/15/12/1484 |
https://repozitorij.uni-lj.si/IzpisGradiva.php?id=142958 |
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Database name | Field | Year |
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Links to authors' personal bibliographies | Links to information on researchers in the SICRIS system |
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Ábrányi-Balogh, Péter | |
Keeley, Aaron | |
Ferenczy, György G. | |
Petri, László | |
Imre, Tímea | |
Grabrijan, Katarina | 50814 |
Hrast, Martina | 32036 |
Knez, Damijan, farmacevt | 36438 |
Ilaš, Janez | 24400 |
Gobec, Stanislav, 1970- | 15284 |
Keserü M., György |
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