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- Title
Design, synthesis, and biological evaluation of chrysin derivatives as potential FabH inhibitors.
- Authors
Li, Hong ‐ Xia; Wang, Zhong ‐ Chang; Qian, Yu ‐ Mei; Yan, Xiao ‐ Qiang; Lu, Ya ‐ Dong; Zhu, Hai ‐ Liang
- Abstract
New series of chrysin derivatives ( 4a- 4t) were designed and synthesized by introducing different substituted piperazines at C-7 position. Their inhibitory effects on FabH were evaluated using two Gram-negative bacterial strains, Escherichia coli and Pseudomonas aeruginosa, and two Gram-positive bacterial strains, Bacillus subtilis and Staphylococcus aureus. To our delight, most of these compounds exhibited a dramatic increase in inhibitory potency, compared with the control positive drugs. Among them, compound 4s exhibited the most potent inhibitory activity with IC50 values of 5.78 ± 0.24 μ m inhibiting E. coli FabH and potent antibacterial activity against S. aureus and E. coli with MIC of 1.25 ± 0.01, 1.15 ± 0.12 μg/mL, respectively, comparing to the control positive drugs penicillin G (7.56 ± 0.30 μ m). Docking simulation was performed to position compound 4s into the FabH active site, and the result showed that compound 4s could bind well with the FabH as potent FabH inhibitor.
- Subjects
FLAVONOIDS; CARRIER proteins; ORGANIC synthesis; DRUG design; MOLECULAR docking
- Publication
Chemical Biology & Drug Design, 2017, Vol 89, Issue 1, p136
- ISSN
1747-0277
- Publication type
Article
- DOI
10.1111/cbdd.12839