Abstract
5-Substituted 7-amino-4,5-tetrahydrothieno[2,3-c]pyridines and 6-substituted 4-amino-6,7-dihydrothieno[3,2-c]pyridines were shown to be exceptionally potent inhibitors of inducible and neuronal nitric oxide synthase. Selectivity and potency could be modulated by variation of the 5- or 6-substituent. Compound 3e showed potent in vivo inhibition of iNOS.
MeSH terms
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Animals
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Blood Pressure / drug effects
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Cells, Cultured
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Cerebellum / cytology
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Cyclopropanes / chemical synthesis
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Cyclopropanes / pharmacology*
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Enzyme Inhibitors / chemical synthesis
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Enzyme Inhibitors / pharmacology
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Humans
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In Vitro Techniques
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Inhibitory Concentration 50
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Lipopolysaccharides / pharmacology
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Models, Animal
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Nitric Oxide Synthase / antagonists & inhibitors*
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Nitric Oxide Synthase Type I
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Nitric Oxide Synthase Type II
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Nitrites / agonists
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Pyridines / chemical synthesis
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Pyridines / pharmacology*
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Rats
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omega-N-Methylarginine / pharmacology
Substances
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Cyclopropanes
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Enzyme Inhibitors
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Lipopolysaccharides
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Nitrites
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Pyridines
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omega-N-Methylarginine
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NOS1 protein, human
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NOS2 protein, human
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Nitric Oxide Synthase
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Nitric Oxide Synthase Type I
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Nitric Oxide Synthase Type II
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Nos1 protein, rat
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Nos2 protein, rat