Watanabe H, Menzies J A, Jordan N, Loo J C
Res Commun Chem Pathol Pharmacol. 1981 Mar;31(3):435-42.
Co-administration of isonicotinic acid hydrazide (isoniazid, INH) and 17 alpha-ethinyl-17 beta-hydroxyestr-4-en-3-one (norethindrone, NE) resulted in the formation of the isonicotinyl hydrazone of norethindrone (INH-NE) in rat stomach. Rat liver metabolized the latter compound in vitro. The metabolic product was characterized, following its derivatization with p-methoxy-benzaldehyde (PMBA), by comparison of chromatographic and mass spectral properties with synthetic reference compound. Results showed that INH-NE was cleaved at the amide bond resulting in the formation of the hydrazone of norethindrone. The physicochemical characteristics of synthetic PMBA hydrazone of norethindrone are described.
异烟肼（INH）与炔诺酮（NE，17α-乙炔基-17β-羟基雌甾-4-烯-3-酮）在大鼠胃中共同给药后，形成了炔诺酮异烟腙（INH-NE）。大鼠肝脏在体外对后一种化合物进行了代谢。在用对甲氧基苯甲醛（PMBA）衍生化后，通过将色谱和质谱特性与合成参考化合物进行比较，对代谢产物进行了表征。结果表明，INH-NE在酰胺键处断裂，生成了炔诺酮腙。描述了合成的炔诺酮PMBA腙的物理化学特性。
