Abstract
New anti-Helicobacter pylori (H. pylori) agents endowed with H2-antagonists properties were obtained by combining the lamtidine derived pharmacophoric group with the antibiotic calvatic acid. All the compounds were tested for their irreversible H2-antagonist properties and for their ability to inhibit 20 H. pylori strains, two of them metronidazole resistant. The most active derivative (compound 4) displayed antimicrobial activity similar to metronidazole.
Publication types
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Comparative Study
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Research Support, Non-U.S. Gov't
MeSH terms
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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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Benzoates / chemistry
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Benzoates / pharmacology
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Binding, Competitive
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Combinatorial Chemistry Techniques
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Dose-Response Relationship, Drug
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Drug Resistance
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Guinea Pigs
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Heart Atria / chemistry
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Helicobacter pylori / drug effects*
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Histamine / metabolism
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Histamine H2 Antagonists / chemical synthesis*
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Histamine H2 Antagonists / pharmacology
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Metronidazole / pharmacology
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Microbial Sensitivity Tests
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Nitriles / chemistry
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Nitriles / pharmacology
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Piperidines / chemistry
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Piperidines / pharmacology
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Receptors, Histamine H2 / metabolism
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Structure-Activity Relationship
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Triazoles / chemistry
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Triazoles / pharmacology
Substances
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Anti-Bacterial Agents
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Benzoates
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Histamine H2 Antagonists
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Nitriles
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Piperidines
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Receptors, Histamine H2
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Triazoles
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Metronidazole
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calvatic acid
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Histamine
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lamtidine