Abstract
1H-Pyrazole-1-carboxamidines were prepared as potential inhibitors of the three isozymes of nitric oxide synthase. All of the compounds were found to be competitive inhibitors of all three isoforms. The most selective compound prepared was 1H-pyrazole-N-(3-aminomethylanilino)-1-carboxamidine (14), which is 100-fold selective for nNOS over eNOS with a Ki value of 2 microM.
Publication types
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Amidines / chemical synthesis
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Amidines / pharmacology
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Animals
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Cattle
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / pharmacology
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Isoenzymes / antagonists & inhibitors
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Isoenzymes / isolation & purification
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Mice
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Molecular Conformation
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Nitric Oxide Synthase / antagonists & inhibitors*
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Nitric Oxide Synthase / isolation & purification
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Nitric Oxide Synthase Type II
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Protein Binding
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Pyrazoles / chemical synthesis
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Pyrazoles / pharmacology
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Rats
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Structure-Activity Relationship
Substances
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Amidines
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Enzyme Inhibitors
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Isoenzymes
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Pyrazoles
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Nitric Oxide Synthase
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Nitric Oxide Synthase Type II
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Nos2 protein, mouse
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Nos2 protein, rat