Abstract
The influence of aromatic substitution on a newly discovered class of inhibitors of dipeptidyl peptidase IV was investigated. A 10(5)-fold increase in potency was achieved by the optimization of aromatic substituents in a parallel chemistry program. The observed SAR could be explained by an X-ray structure of the protein-ligand complex.
MeSH terms
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Adenosine Deaminase / metabolism
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Adenosine Deaminase Inhibitors*
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Glycoproteins / antagonists & inhibitors*
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Glycoproteins / metabolism
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Protease Inhibitors / chemistry*
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Protease Inhibitors / metabolism
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Pyrimidines / chemistry*
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Pyrimidines / metabolism
Substances
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Adenosine Deaminase Inhibitors
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Glycoproteins
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Protease Inhibitors
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Pyrimidines
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Adenosine Deaminase