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.
Keywords:
8-Amino imidazo[1,2-a]pyrazine; ATPase inhibitor; Bacterial type IV secretion system; HP0525.
Copyright © 2014 The Authors. Published by Elsevier Ltd.. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Anti-Bacterial Agents / chemical synthesis
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Anti-Bacterial Agents / chemistry*
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Anti-Bacterial Agents / metabolism
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Bacterial Proteins / antagonists & inhibitors*
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Bacterial Proteins / metabolism
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Binding Sites
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Gram-Negative Bacteria / metabolism
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Imidazoles / chemical synthesis
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Imidazoles / chemistry*
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Imidazoles / metabolism
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Kinetics
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Molecular Docking Simulation
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Protein Binding
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Protein Structure, Tertiary
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Pyrazines / chemical synthesis
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Pyrazines / chemistry*
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Pyrazines / metabolism
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Structure-Activity Relationship
Substances
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Anti-Bacterial Agents
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Bacterial Proteins
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Imidazoles
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Pyrazines
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imidazo(1,2-a)pyrazine