Studies On Prodrug Design, Synthesis And Biological Activity Of Bioactive Cyclovirobuxine D

With the increase of patients suffered from cardiovascular disease, the disease's mechanism and treatment study were paid attention by the medical science and whole society. Cyclovirobuxine D separated from plant foliole box was the availability component of steroid alkaloid and possessed various biological activities. The pharmacological tests and clinical observations showed that cyclovirobuxine D can cure heart failure, angina, arrhythmia, etc. But its bad solubility and poor biological utilization limited the abroad and availability use of cyclovirobuxine D deeply. Therefore it is significant to design and synthesize cyclovirobuxine D derivatives with better curative effect and more expanded safety treatment scope by structure modification on cyclovirobuxine D. It is a pity few studies on this work were found in the literature so far.In this paper, two series of cyclovirobuxine D derivatives, 16 target compounds were designed and synthesized: (1) the sulfonamide derivatives of cyclovirobuxine D; (2) the PEGylated derivatives of cyclovirobuxine D. The structures were all confirmed by 1HNMR and IR. The first series were also confirmed by MS and HRMS. The 16 target compounds have never been reported before.All target compounds of preliminary investigation on the bioactivity have been carried out to test our designs. The results of bioactivity of these target compounds showed that all of the sulfonamide derivatives have good endurance lacking oxygen activity, and especially 3,20-N methyl sulfonamide derivative and 20-N-2,4,6...