Design, Synthesis and Biological Evaluation of Lipophilic Analogs of Anethol Trithione

被引：2

作者：

Li, Xiao-Cen ^{[2
]}

Fan, Wei ^{[2
]}

Hai, Li ^{[2
]}

Qian, Shan ^{[2
]}

Xiao, Qui-Qi ^{[1
]}

Guan, Mei ^{[1
]}

机构：

[1] Sichuan Univ, W China Hosp, Chengdu 610041, Sichuan, Peoples R China

[2] Sichuan Univ, W China Sch Pharm, Key Lab Drug Targeting, Chengdu 610041, Sichuan, Peoples R China

来源：

LETTERS IN DRUG DESIGN & DISCOVERY | 2010年 / 7卷 / 10期

关键词：

Synthesis; Anethol trithione; Lipophilicity; Bioavailability; Prodrugs;

D O I：

10.2174/1570180811007010747

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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.

引用

页码：747 / 753

页数：7

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