Novel 5α-reductase inhibitors. Synthesis and structure-activity studies of 5-substituted 1-methyl-2-pyridones and 1-methyl-2-piperidones

RW Hartmann, M Reichert, S Göhring

Index: Hartmann, R. W.; Reichert, M.; Goehring, S. European Journal of Medicinal Chemistry, 1994 , vol. 29, # 11 p. 807 - 818

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Citation Number: 33

Abstract

Abstract In search for nonsteroidal inhibitors of 5α-reductase for the treatment of benign prostatic hyperplasia (BPH) and possibly prostate cancer, substrate mimicks were synthesized comprising of a 1-methyl-2-pyridone (2, 4–16) or 1-methyl-2-piperidone (1, 3, 17–22) moiety (mimicking steroidal ring A) and a diisopropyl (1, 2,(E)-5-(E)-7,(Z)-5-(Z)-7, 11– 13, 17–19) or a tert-butyl (3, 4,(E)-8-(E)-10,(Z)-8-(Z)-10, 14–16, 20–22) benzamide ( ...