Abstract
The synthesis and in vitro optimization of the anti-Helicobacter pylori activity of a novel series of benzyloxyisoquinoline derivatives discovered by a random screening process, are described. FR180102 (7f), having a 3-acetamido-2,6-dichlorobenzyl moiety, was found to have extremely potent activity against H. pylori and no effect against a series of common Gram-positive and Gram-negative bacteria.
MeSH terms
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Acetamides / chemical synthesis
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Acetamides / chemistry
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Acetamides / pharmacology*
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Animals
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Anti-Bacterial Agents / chemical synthesis
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Anti-Bacterial Agents / chemistry
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Anti-Bacterial Agents / pharmacology*
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Helicobacter pylori / drug effects*
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Isoquinolines / chemical synthesis
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Isoquinolines / chemistry
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Isoquinolines / pharmacology*
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Magnetic Resonance Spectroscopy
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Mice
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Microbial Sensitivity Tests
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Structure-Activity Relationship
Substances
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Acetamides
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Anti-Bacterial Agents
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FR 180102
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Isoquinolines