Identification and synthesis of an efficient multivalent E. coli heat labile toxin inhibitor
- Resource Type
- Authors
- Jintao, Xu; Shixin, Zhang; Shuang, Zhao; Lei, Hu
- Source
- Bioorganicmedicinal chemistry. 28(9)
- Subject
- Aldehydes
Dose-Response Relationship, Drug
Molecular Structure
Cell Survival
Escherichia coli Proteins
Bacterial Toxins
Galactose
Cell Line
Enterotoxins
Structure-Activity Relationship
Hydrazines
Propylene Glycols
Combinatorial Chemistry Techniques
Humans
- Language
- ISSN
- 1464-3391
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.