1258508-97-2Relevant academic research and scientific papers
Design synthesis and biological evaluation of lipophilic analogs of anethol trithione
Li, Xiao-Cen,Fan, Wei,Hai, Li,Qian, Shan,Xiao, Qui-Qi,Guan, Mei
, p. 747 - 753 (2010)
16 ADT carboxylate esters were prepared and tested for their chemical characteristics, stability, bioavailability, potency and toxicity. Considering the good bioavailability, 3a was selected for the pharmacology test, and the result showed that the potency of 3a was remarkably higher than that of ATT. Additionally, 3a was also chosen for the acute toxicity test. The result indicated that the prodrug 3a was more safer than ATT. The study suggested the feasibility to improve the bioavailability of ATT by using prodrug strategy.
Synthesis and biological evaluation of lipid-soluble prodrugs of anethole dithiolthione
Guan, Mei,Fan, Wei,Qian, Shan,Xiao, Rui Qi,Wu, Yong
experimental part, p. 1427 - 1429 (2011/10/09)
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.
