Abstract: | The abortifacient properties of analogs of aminoglutethimide were tested in rats. Aminoglutethimide is nonsteroidal and nonestrogenic, and induces abortion in pregnant rats by interfering with the conversion of cholesterol to delta5-pregnenolone. However, the spread between efficacy (100 mg/kg) and toxicity (200 mg/kg) is not large, thus limiting its potential use in humans. A series of derivatives, Schiff b ases and an unsaturated ring system were prepared. None of the prepared analogs demonstrated the abortifacient activity of aminoglutethimide. It is concluded that the abortifacient activity of aminoglutethimide is highly specific, and that all changes made caused the activity to be lost. The experimental procedures involved in preparing the analogs are described. |