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Antiandrogen. III. 11-oxapregnane steroids
S Takegawa1, N Koizumi, M Mieda
1Research Department, Teikoku Hormone Mfg. Co. Ltd., Kawasaki, Japan.
Chemical & Pharmaceutical Bulletin
|April 1, 1996
Summary
Two novel antiandrogenic compounds, 11-oxachlormadinone acetate and 2,11-dioxachlormadinone acetate, were synthesized. The latter demonstrated superior antiandrogenic potency in castrated rats compared to chlormadinone acetate.
Area of Science:
- Medicinal Chemistry
- Endocrinology
- Pharmacology
Background:
- Chlormadinone acetate is a known antiandrogenic compound.
- Development of novel antiandrogenic agents is crucial for treating androgen-dependent conditions.
- Structural modification of existing drugs can lead to improved therapeutic profiles.
Purpose of the Study:
- To synthesize and evaluate 11-oxachlormadinone acetate and 2,11-dioxachlormadinone acetate as potential antiandrogenic agents.
- To compare the antiandrogenic potency of these novel compounds with the parent compound, chlormadinone acetate.
Main Methods:
- Chemical synthesis of 11-oxachlormadinone acetate and 2,11-dioxachlormadinone acetate.
- In vivo testing of antiandrogenic activity in castrated rats.
Main Results:
- Both synthesized compounds exhibited antiandrogenic properties.
- 2,11-dioxachlormadinone acetate showed significantly greater antiandrogenic potency than chlormadinone acetate in the castrated rat model.
Conclusions:
- 2,11-dioxachlormadinone acetate represents a promising novel antiandrogenic agent with enhanced potency.
- Further investigation into the pharmacological profile and therapeutic applications of 2,11-dioxachlormadinone acetate is warranted.