Abstract
[structure: see text] The combinatorial parallel synthesis of peptide-biphenyl hybrids on solid support using state of the art of peptide synthesis is reported. Key steps were the N to C addition of an amino moiety, hydrolysis of the methyl ester, and the absence of cross-linked compounds when the 2,2'-diamino-1,1'-biphenyl was incorporated. When tested for activity as calpain inhibitors, some of the compounds exhibited IC(50) values in the nanomolar range.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Amino Acid Sequence
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Amino Acids / chemistry
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Biphenyl Compounds / chemical synthesis*
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Biphenyl Compounds / pharmacology
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Calpain / antagonists & inhibitors*
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Esters / chemistry
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Hydrolysis
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Molecular Structure
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Peptides / chemical synthesis*
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Peptides / pharmacology
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Protease Inhibitors / chemical synthesis*
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Protease Inhibitors / pharmacology
Substances
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Amino Acids
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Biphenyl Compounds
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Esters
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Peptides
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Protease Inhibitors
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Calpain