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|Scopus||Web of Science®||Altmetric|
|Title:||Evaluation of 4'-substituted bicyclic pyridones as non-steroidal inhibitors of steroid 5a-reductase|
|Citation:||Bioorganic & Medicinal Chemistry Letters, 2007; 17(13):3603-3607|
|Publisher:||Pergamon-Elsevier Science Ltd|
|Anna R. McCarthy, Rolf W. Hartmann and Andrew D. Abell|
|Abstract:||4′-Substituted bicyclic pyridones were prepared and evaluated as non-steroidal inhibitors of type 1 and 2 steroid 5greek small letter alpha-reductase (SR). A range of 4′-substituents were incorporated into the bicyclic scaffold to investigate SAR within and across different classes of non-steroidal inhibitors of SR. Bicyclic pyridones containing a 4′-benzoyl or long carbon chain tether showed more potent inhibition against type 1 SR than inhibitors with N-substituted acetamide groups in the 4′-position. SAR derived from 4′-substituted bicyclic pyridones reported here do not correlate with SAR derived from known potent 4′-substituted biaryl acid SR inhibitors. A 4′-benzoyl group is favoured by the active site in both isozymes.|
|Keywords:||Kidney; Cell Line; Humans; Carbon; Pyridones; Steroids; Protein Isoforms; Enzyme Inhibitors; Inhibitory Concentration 50; Binding Sites; Structure-Activity Relationship; Drug Design; Chemistry, Pharmaceutical; Models, Chemical; 3-Oxo-5-alpha-Steroid 4-Dehydrogenase; 5-alpha Reductase Inhibitors|
|Appears in Collections:||Chemistry and Physics publications|
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