Shibata K, Takegawa S, Koizumi N, Yamakoshi N, Shimazawa E
Research Department, Teikoku Hormone Mfg. Co., Ltd., Kawasaki, Japan.
Chem Pharm Bull (Tokyo). 1992 Apr;40(4):935-41. doi: 10.1248/cpb.40.935.
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.
2-氮杂氯地孕酮醋酸酯(5α,17-乙酰氧基-6-氯-2-氮杂孕甾-4,6-二烯-3,20-二酮)、2-氧杂氯地孕酮醋酸酯(6,17-乙酰氧基-6-氯-2-氧杂孕甾-4,6-二烯-3,20-二酮)及其衍生物被制备作为潜在的抗雄激素剂。生物学评价表明,5α和6在去势雄性大鼠中测试时具有强效抗雄激素活性。