Evaluation of 4′-substituted bicyclic pyridones as non-steroidal inhibitors of steroid 5α-reductase

AR McCarthy, RW Hartmann, AD Abell

Index: McCarthy, Anna R.; Hartmann, Rolf W.; Abell, Andrew D. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 13 p. 3603 - 3607

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Citation Number: 14

Abstract

4′-Substituted bicyclic pyridones were prepared and evaluated as non-steroidal inhibitors of type 1 and 2 steroid 5α-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 ...