Antiandrogen. I. 2-Azapregnane and 2-Oxapregnane Steroids

Kenyu SHIBATA; Shigehiro TAKEGAWA; Naoyuki KOIZUMI; Nobuaki YAMAKOSHI; Eiichiro SHIMAZAWA

doi:10.1248/cpb.40.935

Kenyu SHIBATA, Shigehiro TAKEGAWA, Naoyuki KOIZUMI, Nobuaki YAMAKOSHI, Eiichiro SHIMAZAWA

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Keywords: antiandrogen, ventral prostate, cholormadinone acetate, 2-azachlormadinone acetate, 2-oxachlormadinone acetate, osmium oxidation, reductive amination, ozonolysis, structure-activity relationship

JOURNAL FREE ACCESS

1992 Volume 40 Issue 4 Pages 935-941

DOI https://doi.org/10.1248/cpb.40.935

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Abstract

2-Azachlormadinone acetate (5a, 17-acetoxy-6-chloro-2-azapregna-4, 6-diene-3, 20-dione), 2-oxachlormadinone acetate (6, 17-acetoxy-6-chloro-2-oxapregna-4, 6-diene-3, 20-dione) and the derivatives were prepared as potential antiandrogenic agents. Biological evaluation showed that 5a and 6 had a potent antiandrogenic activity when tested in the castrated male rat.

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