Abstract
A novel alpha-addition of propiolates to urazoles followed by Michael addition of a variety of nucleophiles has been developed for rapid production and optimization of peptidomimetic drug leads. This technology has produced a number of highly potent and selective inhibitors of the serine protease, thrombin.
MeSH terms
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Alkynes / chemistry
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Combinatorial Chemistry Techniques
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Molecular Mimicry
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Propionates / chemistry
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Serine Proteinase Inhibitors / chemical synthesis
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Serine Proteinase Inhibitors / pharmacology
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Structure-Activity Relationship
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Thrombin / antagonists & inhibitors*
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Triazoles / chemical synthesis*
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Triazoles / chemistry
Substances
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Alkynes
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Propionates
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Serine Proteinase Inhibitors
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Triazoles
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Thrombin
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propiolic acid
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urazole