引用本文:
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
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
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
Synthesis and biological evaluation of lipid-soluble prodrugs of anethole dithiolthione
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.
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关键词:
- Synthesis
- / Anethole dithiolthione
- / Liposoluble
- / Bioavailability
- / Prodrug
English
Synthesis and biological evaluation of lipid-soluble prodrugs of anethole dithiolthione
Abstract:
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.
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Key words:
- Synthesis
- / Anethole dithiolthione
- / Liposoluble
- / Bioavailability
- / Prodrug
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