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Lead detoxification activities and ADMET hepatotoxicities of a class of novel 5-(1-carbonyl-L-amino-acid)-2,2-dimethyl-[1,3]dithiolane-4-carboxylic acids
Xu, Yanxia2; Wang, Yuji1; Zhao, Ming1; Hou, Baoguang1; Peng, Li1; Zheng, Meiqing1; Wu, Jianhui1; Peng, Shiqi1,2
关键词Dmsa Structural Modification Brain Lead Detoxification
刊名BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
2011-03-15
DOI10.1016/j.bmcl.2011.01.070
21期:6页:1754-1757
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Chemistry, Medicinal ; Chemistry, Organic
资助者PHR ; National Natural Scientific Foundation of China ; Special Project of China ; PHR ; National Natural Scientific Foundation of China ; Special Project of China
研究领域[WOS]Pharmacology & Pharmacy ; Chemistry
关键词[WOS]INDUCED OXIDATIVE STRESS ; GILL TISSUES ; EXPOSURE ; DMSA ; RATS
英文摘要

By linking the mercapto groups with isopropyl and introducing L-amino acid into the 5-carboxyl of DMSA a class of novel 5-(1-carbonyl-L-amino-acid)-2,2-dimethyl-[1,3]dithiolane-4-carboxylic acids were prepared. Their in vivo activities were evaluated on lead loaded mice at the dose of 0.4 mmol/kg. The results showed that the lead levels of the livers, kidneys, femurs and brains in particular could be efficiently decreased by 0.4 mmol/kg of 5-(1-carbonyl-L-amino-acid)-2,2-dimethyl-[1,3] dithiolane-4-carboxylic acids. The benefit of 5-(1-carbonyl-L-amino-acid)-2,2-dimethyl-[1,3] dithiolane-4-carboxylic acids to the detoxification of the brain lead was attributed to their transmembrane ability. Compared with the lead detoxification efficacy, they did not affect the essential metals such as Fe, Cu, Zn, and Ca of the treated mice. Silico molecular modeling predicted that 5-(1-carbonyl-L-amino-acid)-2,2-dimethyl-[1,3]dithiolane-4-carboxylic acids had no hepatotoxicity. Crown Copyright (C) 2011 Published by Elsevier Ltd. All rights reserved.

语种英语
所属项目编号KZ200810025010 ; KM200910025009 ; KM200710025010 ; 30801426 ; 2008ZX09401-002
资助者PHR ; National Natural Scientific Foundation of China ; Special Project of China ; PHR ; National Natural Scientific Foundation of China ; Special Project of China
WOS记录号WOS:000288012800040
Citation statistics
Cited Times:4[WOS]   [WOS Record]     [Related Records in WOS]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/57639
Collection北京大学药学院
作者单位1.Capital Med Univ, Coll Pharmaceut Sci, Beijing 100069, Peoples R China
2.Peking Univ, Coll Pharmaceut Sci, Beijing 100083, Peoples R China
Recommended Citation
GB/T 7714
Xu, Yanxia,Wang, Yuji,Zhao, Ming,et al. Lead detoxification activities and ADMET hepatotoxicities of a class of novel 5-(1-carbonyl-L-amino-acid)-2,2-dimethyl-[1,3]dithiolane-4-carboxylic acids[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2011,21(6):1754-1757.
APA Xu, Yanxia.,Wang, Yuji.,Zhao, Ming.,Hou, Baoguang.,Peng, Li.,...&Peng, Shiqi.(2011).Lead detoxification activities and ADMET hepatotoxicities of a class of novel 5-(1-carbonyl-L-amino-acid)-2,2-dimethyl-[1,3]dithiolane-4-carboxylic acids.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,21(6),1754-1757.
MLA Xu, Yanxia,et al."Lead detoxification activities and ADMET hepatotoxicities of a class of novel 5-(1-carbonyl-L-amino-acid)-2,2-dimethyl-[1,3]dithiolane-4-carboxylic acids".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 21.6(2011):1754-1757.
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