Abstract
The reported diketopiperazine calpain inhibitor, cis-L-L-3,6-bis-(4-hydroxybenzyl)-1,4-dimethylpiperazine-2,5-dione 1, and its analogues 3 and 4 were synthesized from the corresponding amino acids. The previously assigned structure of 1 is confirmed but neither synthetic 1 nor its N-methylphenylalanine analogues 3 and 4 inhibit porcine erythrocyte calpain I.
Publication types
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Animals
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Calpain / antagonists & inhibitors*
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Calpain / metabolism
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Cysteine Proteinase Inhibitors / chemical synthesis
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Cysteine Proteinase Inhibitors / chemistry
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Cysteine Proteinase Inhibitors / pharmacology
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Erythrocytes / drug effects
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Erythrocytes / enzymology
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Glycoproteins / chemical synthesis*
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Glycoproteins / chemistry
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Glycoproteins / isolation & purification
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Glycoproteins / pharmacology
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Magnetic Resonance Spectroscopy
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Piperazines / chemical synthesis*
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Piperazines / chemistry
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Piperazines / pharmacology
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Streptomyces griseus / chemistry*
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Swine
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Tyrosine / analogs & derivatives*
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Tyrosine / chemical synthesis*
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Tyrosine / chemistry
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Tyrosine / pharmacology
Substances
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3,6-bis(4-hydroxyphenylmethyl)-1,4-dimethyl-2,5-diketopiperazine
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Cysteine Proteinase Inhibitors
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Glycoproteins
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Piperazines
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calpain inhibitors
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Tyrosine
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Calpain