Abstract
Several beta-amino tetrazole analogs of gabapentin 1 and pregabalin 2 were prepared by one of two convergent, highly efficient routes, and their affinity for the alpha(2)-delta protein examined. Two select compounds with potent affinity for alpha(2)-delta, 8a and 16a, were subsequently tested in vivo in an audiogenic seizure model and found to elicit protective effects.
MeSH terms
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Amines / chemical synthesis
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Amines / chemistry
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Amines / pharmacology
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Animals
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Anticonvulsants / chemical synthesis*
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Anticonvulsants / chemistry
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Anticonvulsants / pharmacology*
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Binding Sites
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Carboxylic Acids / chemistry*
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Cyclohexanecarboxylic Acids / chemical synthesis
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Cyclohexanecarboxylic Acids / chemistry
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Cyclohexanecarboxylic Acids / pharmacology
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Disease Models, Animal
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Drug Evaluation, Preclinical
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Epilepsy, Reflex / prevention & control*
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Gabapentin
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Mice
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Mice, Inbred DBA
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Molecular Structure
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Pregabalin
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Protein Subunits / drug effects
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Stereoisomerism
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Structure-Activity Relationship
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gamma-Aminobutyric Acid / analogs & derivatives*
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gamma-Aminobutyric Acid / chemical synthesis
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gamma-Aminobutyric Acid / chemistry
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gamma-Aminobutyric Acid / pharmacology
Substances
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Amines
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Anticonvulsants
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Carboxylic Acids
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Cyclohexanecarboxylic Acids
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Protein Subunits
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Pregabalin
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gamma-Aminobutyric Acid
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Gabapentin