Über die adrenale Steroid‐Biosynthese in vitro. III. Selektive Hemmung der Nebennierenrinden‐Funktion

Abstract

AbstractThe possibility is discussed of inhibiting the adrenocortical functions either selectively or preferentially by blocking the hydroxylations in positions 11β, 17α, 18 and 19 of the steroid nucleus or in 20α, 21 and 22 of the side chain, which are necessary for the formation of the individual corticosteroids from cholesterol. Many compounds with or without other biological activities, such as o,p′‐DDD, Amphenone B, various blockers of cholesterol biosynthesis, heparinoids and various heterocyclic compounds, are shown to be devoid of a specific blocking activity on the adrenal cortex in vitro. However, amongst a large group of glutaric imides a few compounds proved to be active, mainly by blocking the 20α‐hydroxylation of cholesterol, the most active being a cyclic hydrazide; the secretion in vivo of corticosteroids greatly decreased in response to 3–20 mg/kg. A new class of compounds active in vitro was found among simple imidazole derivatives, which block 17α, 18 and 19‐hydroxylation.