Hsu S Y, Huang C L, Waters I W
J Med Chem. 1975 Jan;18(1):20-3. doi: 10.1021/jm00235a004.
The effect of incorporation of an eleostearoyl group into molecules of aralkylhydrazines on their monoamine oxidase inhibitory potency was investigated in vitro and in vivo. The results showed that on a molar basis the hydrazides possessed an in vitro potency lower than and an in vivo potency and acute toxicity comparable to those of the corresponding aralkylhydrazines. The sequence of the relative potency of aralkylhydrazines and their hydrazides was similar. The overall pharmacological profile indicated that these aralkylhydrazines retained their monoamine oxidase inhibitory properties when the free hydrazine nitrogen was acylated with an eleostearoyl group.
研究了将桐酰基引入芳烷基肼分子中对其单胺氧化酶抑制效力的影响，进行了体外和体内实验。结果表明，以摩尔计，酰肼的体外效力低于相应的芳烷基肼，但其体内效力和急性毒性与之相当。芳烷基肼及其酰肼的相对效力顺序相似。整体药理学特征表明，当游离肼氮被桐酰基酰化后，这些芳烷基肼仍保留其单胺氧化酶抑制特性。
