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Identification and synthesis of an efficient multivalent E. coli heat labile toxin inhibitor __ A dynamic
Jintao Xu1, Shixin Zhang1, Shuang Zhao1
1School of Pharmacy, Jiangsu University, Zhenjiang, China.
Abstract:
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.
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