Abstract
In an attempt to find new compounds with neuroprotective activity, we have designed, synthesized and characterized 19 new nNOS inhibitors with a 4,5-dihydro-1H-pyrazole structure. Compounds 11r [1-cyclopropanecarbonyl-3-(2-amino-5-chlorophenyl)-4,5-dihydro-1H-pyrazole] and 11e [1-cyclopropanecarbonyl-3-(2-amino-5-methoxyphenyl)- 4,5-dihydro-1H-pyrazole] show the highest activities with inhibition percentages of 70% and 62%, respectively. A structure-activity relationship for the nNOS inhibition can be established from the structural comparison of these new pyrazole derivatives and the described synthetic kynurenines 10.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Aniline Compounds / chemical synthesis*
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Aniline Compounds / chemistry
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Aniline Compounds / pharmacology
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Animals
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Corpus Striatum / drug effects*
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Corpus Striatum / enzymology
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In Vitro Techniques
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Kynurenine / analogs & derivatives
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Kynurenine / chemistry
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Kynurenine / pharmacology
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Models, Molecular
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Molecular Conformation
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Nitric Oxide Synthase / antagonists & inhibitors*
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Nitric Oxide Synthase Type I
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Pyrazoles / chemical synthesis*
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Pyrazoles / chemistry
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Pyrazoles / pharmacology
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Rats
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Structure-Activity Relationship
Substances
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1-cyclopropanecarbonyl-3-(2-amino-5-chlorophenyl)-4,5-dihydro-1H-pyrazole
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1-cyclopropanecarbonyl-3-(2-amino-5-methoxyphenyl)-4,5-dihydro-1H-pyrazole
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Aniline Compounds
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Pyrazoles
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Kynurenine
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Nitric Oxide Synthase
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Nitric Oxide Synthase Type I
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Nos1 protein, rat