Design, synthesis, and evaluation of curcumin analogues as potential inhibitors of bacterial sialidase
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- Design, synthesis, and evaluation of curcumin analogues as potential inhibitors of bacterial sialidase
- Bo Ram Kim; Ji Young Park; Hyung Jae Jeong; Hyung Jun Kwon; Su-Jin Park; In Chul Lee; Young Bae Ryu; Woo Song Lee
- Bibliographic Citation
- Journal of Enzyme Inhibition and Medicinal Chemistry, vol. 33, pp. 1256-1265
- Publication Year
- 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 μM). 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.
- Curcumin; Nan A; sepsis; sialidase
- T&F (Taylor & Francis)
- Appears in Collections:
- Jeonbuk Branch Institute > Functional Biomaterial Research Center > 1. Journal Articles
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