Synthesis and biological evaluation of lipid-soluble prodrugs of anethole dithiolthione  

作　　者：Mei Guan Wei Fan Shan Qian Rui Qi Xiao Yong Wu 

机构地区：[1]West China Hospital, Sichuan University, Chengdu 610041, China [2]Key Laboratory of Drug Targeting of China Education Ministry, West China School of Pharmacy, Sichuan University, Chengdu 610041, China

出　　处：《Chinese Chemical Letters》2010年第12期1427-1429,共3页中国化学快报（英文版）

摘　　要：16 ADT carboxylate esters were prepared by means of esterification and these compounds were expected to increase the bioavailability of 4-hydroxyanehole trithione.In vivo studies showed that ADT concentration of 3a in plasma was much higher than that of ATT during 120 min.Compound 3a could reach blood peak values of ADT at 660.6 ng/mL which was about 14 times of that by ATT.Additionally,the acute toxicity assay indicated high safety of compound 3a that the maximum tolerated dose was no less than 3.25 g/kg.16 ADT carboxylate esters were prepared by means of esterification and these compounds were expected to increase the bioavailability of 4-hydroxyanehole trithione.In vivo studies showed that ADT concentration of 3a in plasma was much higher than that of ATT during 120 min.Compound 3a could reach blood peak values of ADT at 660.6 ng/mL which was about 14 times of that by ATT.Additionally,the acute toxicity assay indicated high safety of compound 3a that the maximum tolerated dose was no less than 3.25 g/kg.

关 键 词：SYNTHESIS Anethole dithiolthione Liposoluble BIOAVAILABILITY PRODRUG 

分 类 号：TQ460.4[化学工程—制药化工] X826[环境科学与工程—环境工程]