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Identification and Synthesis of an Efficient Multivalent E. coli Heat Labile Toxin Inhibitor __ A Dynamic Combinatorial Chemistry Approach
Bioorganic & Medicinal Chemistry ( IF 3.5 ) Pub Date : 2020-03-13 , DOI: 10.1016/j.bmc.2020.115436
Jintao Xu 1 , Shixin Zhang 1 , Shuang Zhao 1 , Lei Hu 1
Affiliation  

A polymer based dynamic combinatorial library (DCL) was generated through condensation between aldehyde functionalized linear poly(glycidol) (APG) and galactose containing acylhydrazide derivatives. Pentameric E. coli heat labile enterotoxin B subunit (LTB) was subsequently applied to the DCL as external stimulus, resulting in amplification of a specific acylhydrazone side chain that was further used for the synthesis of a multivalent LTB inhibitor. In the in vitro biological evaluation, this inhibitor exhibited strong inhibition properties as well as low cytotoxicity.



中文翻译:

一种高效多价大肠杆菌热不稳定毒素抑制剂的鉴定和合成__动态组合化学方法

通过醛官能化线性聚缩水甘油 ( APG ) 和含有酰肼衍生物的半乳糖之间的缩合生成基于聚合物的动态组合库 (DCL) 。随后将五聚大肠杆菌热不稳定肠毒素 B 亚基 (LTB) 作为外部刺激应用于 DCL,导致特定酰腙侧链的扩增,该侧链进一步用于合成多价 LTB 抑制剂。在体外生物学评价中,该抑制剂表现出很强的抑制特性以及低细胞毒性。

更新日期:2020-03-16
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