Citation: Mei Guan, Wei Fan, Shan Qian, Rui Qi Xiao, Yong Wu. Synthesis and biological evaluation of lipid-soluble prodrugs of anethole dithiolthione[J]. Chinese Chemical Letters, ;2010, 21(12): 1427-1429. doi: 10.1016/j.cclet.2010.07.014 shu

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

Mei Guan ^a, ,
Wei Fan ^b ,
Shan Qian ^b ,
Rui Qi Xiao ^b ,
Yong Wu ^b

a West China Hospital, Sichuan University, Chengdu 610041, China;
b Key Laboratory of Drug Targeting of China Education Ministry, West China School of Pharmacy, Sichuan University, Chengdu 610041, China

Received Date: 23 March 2010

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.
- Synthesis,
- Anethole dithiolthione,
- Liposoluble,
- Bioavailability,
- Prodrug
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