Varga S V, Reznikov A G, Bal'on Ia G, Lozinskiĭ M O, Smirnov V A
Probl Endokrinol (Mosk). 1983 Mar-Apr;29(2):67-71.
The synthesis of 10 substituted carboxy anilides was performed and their antiandrogenic activity was investigated. It was shown, that 4-nitro-3-trifluoro-methyl-alpha-hydroxy-isobutyranilide, 4-nitro-3-trifluoro-methyl-isobutyranilide and 4-nitro-3-trifluoro-methyl-ethyl-methyl acetanilide exert the most pronounced antiandrogenic effects in experimental immature castrated male rats, given substituted doses of testosterone propionate. The antiandrogenic activity is mainly caused by the presence of trifluoro-methyl- and nitro-groups in meta- and para-positions of anilide benzene ring, as well as by hydroxyl group and hydrogen atom presence in alpha-carbon atom of the molecule alkyl moiety. A possible use of non-steroid antiandrogens for studying androgen mechanism of action and treating androgen-dependent diseases is discussed.
合成了10种取代羧基苯胺，并研究了它们的抗雄激素活性。结果表明，在给予不同剂量丙酸睾酮的实验性未成熟去势雄性大鼠中，4-硝基-3-三氟甲基-α-羟基异丁酸苯胺、4-硝基-3-三氟甲基异丁酸苯胺和4-硝基-3-三氟甲基-乙基-甲基乙酰苯胺具有最显著的抗雄激素作用。抗雄激素活性主要是由于苯胺苯环间位和对位存在三氟甲基和硝基，以及分子烷基部分α碳原子上存在羟基和氢原子。讨论了非甾体抗雄激素在研究雄激素作用机制和治疗雄激素依赖性疾病方面的可能用途。
