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2- and 3-substituted imidazo[1,2-a]pyrazines as inhibitors of bacterial type IV secretion

Sayer, JR; Walldén, K; Pesnot, T; Campbell, F; Gane, PJ; Simone, M; Koss, H; ... Tabor, AB; + view all (2014) 2- and 3-substituted imidazo[1,2-a]pyrazines as inhibitors of bacterial type IV secretion. Bioorganic and Medical Chemistry , 22 (22) pp. 6459-6470. 10.1016/j.bmc.2014.09.036. Green open access

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Abstract

A novel series of 8-amino imidazo[1,2-a]pyrazine derivatives has been developed as inhibitors of the VirB11 ATPase HP0525, a key component of the bacterial type IV secretion system. A flexible synthetic route to both 2- and 3-aryl substituted regioisomers has been developed. The resulting series of imidazo[1,2-a]pyrazines has been used to probe the structure-activity relationships of these inhibitors, which show potential as antibacterial agents.

Type: Article
Title: 2- and 3-substituted imidazo[1,2-a]pyrazines as inhibitors of bacterial type IV secretion
Location: England
Open access status: An open access version is available from UCL Discovery
DOI: 10.1016/j.bmc.2014.09.036
Publisher version: http://dx.doi.org/10.1016/j.bmc.2014.09.036
Language: English
Additional information: Copyright © 2014 The Authors. Published by Elsevier Ltd. This is an open access article under the CC BY license http://creativecommons.org/licenses/by/3.0/).
Keywords: 8-Amino imidazo[1,2-a]pyrazine, ATPase inhibitor, Bacterial type IV secretion system, HP0525, Anti-Bacterial Agents, Bacterial Proteins, Binding Sites, Gram-Negative Bacteria, Imidazoles, Kinetics, Molecular Docking Simulation, Protein Binding, Protein Structure, Tertiary, Pyrazines, Structure-Activity Relationship
UCL classification: UCL
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > Div of Biosciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > Div of Biosciences > Structural and Molecular Biology
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Medical Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Medical Sciences > Div of Medicine
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Medical Sciences > Div of Medicine > Wolfson Inst for Biomedical Research
UCL > Provost and Vice Provost Offices > UCL BEAMS
UCL > Provost and Vice Provost Offices > UCL BEAMS > Faculty of Maths and Physical Sciences
UCL > Provost and Vice Provost Offices > UCL BEAMS > Faculty of Maths and Physical Sciences > Dept of Chemistry
URI: https://discovery.ucl.ac.uk/id/eprint/1456228
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