Abstract
This paper describes some modifications of the heterocyclic ring of 1-N-benzylsubstituted 1,2,3-triazoles, which are effective inhibitors of the arachidonic acid-induced malondialdehyde production in human platelets. The corresponding 1-N-imidazole- or 1-N-1,2,4-triazole-derivatives, with basic properties, preserve the inhibitory enzymatic activity, whilst the C-substituted tetrazole or 1,3,4-oxadiazole derivatives, with a neutral character, show no activity. A close structural relationship between our active compounds and Dazoxiben, a potent selective tromboxane-synthetase inhibitor, was observed.
MeSH terms
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Anti-Inflammatory Agents, Non-Steroidal / chemical synthesis
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Arachidonic Acid
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Arachidonic Acids / metabolism
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Blood Platelets / drug effects
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Blood Platelets / metabolism
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Chemical Phenomena
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Chemistry
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Humans
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In Vitro Techniques
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Isomerism
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Magnetic Resonance Spectroscopy
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Malondialdehyde / metabolism
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Prostaglandin Antagonists / analysis
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Prostaglandin Antagonists / chemical synthesis*
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Triazoles / analysis
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Triazoles / chemical synthesis*
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Triazoles / pharmacology
Substances
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Anti-Inflammatory Agents, Non-Steroidal
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Arachidonic Acids
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Prostaglandin Antagonists
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Triazoles
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Arachidonic Acid
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Malondialdehyde