Thiophene inhibitors of PDE4: crystal structures show a second binding mode at the catalytic domain of PDE4D2.
Bioorganic & Medicinal Chemistry Letters(2011)
摘要
PDE4 inhibitors have been identified as therapeutic targets for a variety of conditions, particularly inflammatory diseases. We have serendipitously identified a novel class of phosphodiesterase 4 (PDE4) inhibitor during a study to discover antagonists of the parathyroid hormone receptor. X-ray crystallographic studies of PDE4D2 complexed to four potent inhibitors reveal the atomic details of how they inhibit the enzyme and a notable contrast to another recently reported thiophene-based inhibitor.
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关键词
Phosphodiesterase inhibitors,PDE4,Thiophene,Crystallography,Gewald reaction
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