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Title 

Design, synthesis, and evaluation of curcumin analogues as potential inhibitors of bacterial sialidase

Authors 

Bo Ram KimJi Young ParkHyung Jae JeongHyung Jun KwonSu-Jin ParkIn Chul LeeYoung Bae RyuWoo Song Lee

Publisher 

Informa Healthcare

Issue Date 

2018

Citation 

Journal of Enzyme Inhibition and Medicinal Chemistry

Keywords 

CurcuminNan Asepsissialidase

Abstract 

Sialidases are key virulence factors that remove sialic acid from the host cell surface glycan, unmasking receptors that facilitate bacterial adherence and colonisation. In this study, we developed potential agents for treating bacterial infections caused by Streptococcus pneumoniae Nan A that inhibit bacterial sialidase using Turmeric and curcumin analogues. Design, synthesis, and structure analysis relationship (SAR) studies have been also described. Evaluation of the synthesised derivatives demonstrated that compound 5e was the most potent inhibitor of S. pneumoniae sialidase (IC50?=?0.2?±?0.1??M). This compound exhibited a 3.0-fold improvement in inhibitory activity over that of curcumin and displayed competitive inhibition. These results warrant further studies confirming the antipneumococcal activity 5e and indicated that curcumin derivatives could be potentially used to treat sepsis by bacterial infections.

ISSN 

1475-6366

Link 

http://dx.doi.org/10.1080/14756366.2018.1488695

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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