Abstract
A new series of phenyl- and heteryl acetamidines were synthesized and evaluated as inhibitors of nitric oxide synthases (NOS). While the N-substitution of the acetamidine moiety with different heterocycles appears to completely destroy the activity, linking the phenyl core preserves it. Moreover, it was observed a strong dependence of the phenylacetamidines potency of action from the length of the alkyl chain that connects the aromatic ring to the acetamidine moiety.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Amidines / chemistry*
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Amidines / metabolism
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Amidines / pharmacology*
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Animals
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Cattle
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Enzyme Inhibitors / chemistry*
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Enzyme Inhibitors / metabolism
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Enzyme Inhibitors / pharmacology*
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Heterocyclic Compounds / chemistry
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Inhibitory Concentration 50
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Ligands
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Mice
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Nitric Oxide Synthase Type II / antagonists & inhibitors*
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Nitric Oxide Synthase Type II / metabolism
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Sf9 Cells
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Spodoptera
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Substrate Specificity
Substances
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Amidines
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Enzyme Inhibitors
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Heterocyclic Compounds
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Ligands
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Nitric Oxide Synthase Type II
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acetamidine