[Anti-androgenic activity of various substituted carboxyanilides]

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.