Hypolipidemic Activity of Phthalimide Derivatives IV: Further Chemical Modification and Investigation of the Hypolipidemic Activity of N-Substituted Imides
作者:James M. Chapman、George H. Cocolas、I.H. Hall
DOI:10.1002/jps.2600721127
日期:1983.11
A further investigation of N-substituted derivatives of phthalimide for hypolipidemic activity has revealed that the chain length, as well as the type of substitution on the N-alkyl chain of phthalimide is critical for biological activity. In these studies the hypolipidemic activity was not improved by extending the chain length beyond five carbon atoms in the alkyl and alkanoic acid series. Imido
对邻苯二甲酰亚胺的N-取代衍生物进行降血脂活性的进一步研究表明,邻苯二甲酰亚胺的链长以及N-烷基链上的取代类型对于生物学活性至关重要。在这些研究中,通过将烷基和链烷酸系列中的碳原子长度延伸超过五个碳原子,并不能改善降血脂活性。除链烷酸,甲基酮和烷基以外的亚氨基氮取代基引起降血脂活性的降低,例如羟基,氨基,羟甲基或甲乙氧基。除了1-N-邻苯二甲酰亚胺基丁-3-酮半脲以外,将侧链的酮基还原为醇以及形成酮基的衍生物没有改善降血脂活性。该化合物表现出比邻苯二甲酰亚胺和1-N-邻苯二甲酰亚胺基丁三-3-酮改善的降胆固醇活性。邻苯二甲酰亚胺的芳族部分的3-位被氨基或硝基取代,以及用吡啶或环己基环取代苯环,导致降血脂活性降低。