Blaszczyk B, Gieldanowski J
Arch Immunol Ther Exp (Warsz). 1976;24(1):159-68.
A number of derivatives of piperidine-2,4,6-trione and oxazine-2,4-dione with cyclohexyl and allyl substituents at their ring were evaluated pharmacologically. Piperidine-2,4,6-trione compounds, regardless of type of substituent, were readily absorbed from the site of their introduction and displayed similar biological activity. Introduction of the N-cyclohexylcarboxamide substituent diminished general toxicity of the derivative and increased anti-inflammatory activity in all tests. The oxazine-4,6-dione derivatives were poorly absorbed. The bis-(1-cyclohexyl-5,5-diallyl-piperidine-2,4,6-trione) derivative, product of condensation of two molecules of a simpler compound, was very well absorbed, strongly toxic, and showed distinct anti-inflammatory activity. Limited correlation between chemical structure and biological activity was noted, supporting the concept that introduction of cyclohexyl and allyl radicals imparts anti-inflammatory and immunosuppressive activity to derivatives of this type.
对一些在其环上带有环己基和烯丙基取代基的哌啶 -2,4,6 -三酮和恶嗪 -2,4 -二酮衍生物进行了药理学评估。无论取代基类型如何，哌啶 -2,4,6 -三酮化合物都能从引入部位迅速吸收，并表现出相似的生物活性。引入N -环己基甲酰胺取代基降低了衍生物的一般毒性，并在所有测试中增强了抗炎活性。恶嗪 -4,6 -二酮衍生物吸收较差。双 -（1 -环己基 -5,5 -二烯丙基 -哌啶 -2,4,6 -三酮）衍生物是两种较简单化合物分子缩合的产物，吸收非常好，毒性很强，并表现出明显的抗炎活性。注意到化学结构与生物活性之间存在有限的相关性，这支持了这样一种观点，即引入环己基和烯丙基自由基可赋予这类衍生物抗炎和免疫抑制活性。
