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Non-steroidal antiandrogens. Design of novel compounds based on an infrared study of the dominant conformation and hydrogen-bonding properties of a series of …

JJ Morris, LR Hughes, AT Glen…

文献索引:Morris; Hughes; Glen; Taylor Journal of Medicinal Chemistry, 1991 , vol. 34, # 1 p. 447 - 455

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被引用次数: 85

摘要

Antiandrogenic activity is observed in anilides containing a tertiary hydroxyl group, and these compounds are used to define a pharmacophore in terms of their physicochemical properties. Infrared spectroscopy shows that these anilides exist in a single conformation, which exerts a powerful influence on the hydrogen-bond donor ability of the hydroxyl group in a model system. Arguments are presented which suggest that hydrogen-bonding ability ...