Abstract
The sulfamic acid phosphotyrosine mimetic was coupled with a previously known malonate template to obtain highly selective and potent inhibitors of HPTPbeta. Potentially hydrolyzable malonate ester functionalities were replaced with 1,2,4-oxadiazoles without a significant effect on HPTPbeta potency.
MeSH terms
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Chemistry, Pharmaceutical / methods*
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Crystallography, X-Ray
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Drug Design
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Hydrogen Bonding
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Hydrolysis
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Models, Chemical
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Models, Molecular
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Molecular Structure
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Nerve Tissue Proteins / antagonists & inhibitors*
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Protein Tyrosine Phosphatases / antagonists & inhibitors*
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Receptor-Like Protein Tyrosine Phosphatases, Class 5
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Structure-Activity Relationship
Substances
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Nerve Tissue Proteins
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Protein Tyrosine Phosphatases
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Receptor-Like Protein Tyrosine Phosphatases, Class 5