Abstract
A series of tripeptide arginine aldehydes was synthesized by replacement of proline with 1,2-disubstituted cyclohexane derivatives in the sequence of D-MePhe-Pro-Arg-H. Based on molecular modeling, further modification of the D-MePhe residue resulted in a potent and selective thrombin inhibitor.
MeSH terms
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Aldehydes
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Amino Acid Sequence
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Antithrombins / chemical synthesis*
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Antithrombins / chemistry
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Antithrombins / pharmacology
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Arginine
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Binding Sites
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Cyclohexanes / chemical synthesis*
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Cyclohexanes / chemistry
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Cyclohexanes / pharmacology
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Indicators and Reagents
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Kinetics
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Models, Molecular
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Molecular Structure
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Oligopeptides / chemical synthesis*
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Oligopeptides / chemistry
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Oligopeptides / pharmacology
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Protein Conformation
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Stereoisomerism
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Structure-Activity Relationship
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Thrombin / metabolism
Substances
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Aldehydes
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Antithrombins
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Cyclohexanes
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Indicators and Reagents
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Oligopeptides
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Arginine
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Thrombin
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