期刊
JOURNAL OF ASIAN NATURAL PRODUCTS RESEARCH
卷 23, 期 2, 页码 123-137出版社
TAYLOR & FRANCIS LTD
DOI: 10.1080/10286020.2020.1713764
关键词
Pleuromutilin derivatives; antibacterial activity; design; synthesis; Gram-positive bacteria
资金
- Research Project of Hebei Administration of Chinese Medicine [2019080]
- Doctor Foundation of Hebei University of Chinese Medicine [BSZ2018006]
- Basic Research Program of Outstanding Young Teachers of Hebei University of Chinese Medicine [YQ2018004]
Novel pleuromutilin derivatives were synthesized and compound 8 showed potent antimicrobial activity against Staphylococcus aureus and Staphylococcus epidermidis. Compound 8 and tiamulin binding to the ribosome pocket demonstrated that more bonds and stronger combination could enhance the antimicrobial activity of the compounds.
We described the design, synthesis and antimicrobial activities of novel pleuromutilin derivatives with substituted piperazine substrate. Minimum inhibitory concentration (MIC) was used to evaluate the activity of the derivatives against six bacteria in vitro, and compound 8 was potent against Staphylococcus aureus and Staphylococcus epidermidis with the MIC value of 0.0625 mu g/ml. 10a and 10 b showed similar activity to positive control drugs (tiamulin, erythromycin) against S. aureus with the MIC value of 0.125 mu g/ml. The binding mode of compound 8 and tiamulin to the ribosome pocket showed the correlation between binding parameters and the antibacterial activity, and more bonds and stronger combination could effectively enhance the activity of compounds.
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