Synthesis, crystal structures, and anti-drug-resistant Staphylococcus aureus activities of novel 4-hydroxycoumarin derivatives.
Four novel 4-hydroxycoumarin derivatives (4-MBH, 3-MBH, 4-MDT and 3-MDT) were successfully synthesized and their structures were verified by single-crystal X-ray crystallography. All target compounds were evaluated for their in vitro antibacterial activity against Staphylococcus aureus (S. aureus ATCC 29213), methicillin-resistant S. aureus (MRSA XJ 75302), vancomycin-intermediate S. aureus (Mu50 ATCC 700699), and USA 300 (Los Angeles County clone, LAC). The minimum inhibitory concentration and time-kill curves were obtained for the test compounds and antibiotics. Among the tested compounds, 3-MBH showed the most potent antibacterial activities.
Department of Pharmacology, School of Pharmacy, The Fourth Military Medical University, Xi'an, China.
Ming-Kai
MK
Li
Jing
J
Li
Bao-Hui
BH
Liu
Ying
Y
Zhou
Xia
X
Li
Xiao-Yan
XY
Xue
Zheng
Z
Hou
Xiao-Xing
XX
Luo
D015110:4-Hydroxycoumarins / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D060326:Chemistry Techniques, Synthetic; D018360:Crystallography, X-Ray; D024881:Drug Resistance, Bacterial / Q000187:drug effects*; D008826:Microbial Sensitivity Tests; D008958:Models, Molecular; D008968:Molecular Conformation; D013211:Staphylococcus aureus / Q000187:drug effects*; D013329:Structure-Activity Relationship; D013997:Time Factors
D015110:4-Hydroxycoumarins; D000900:Anti-Bacterial Agents; C068805:4-hydroxycoumarin
4-Hydroxycoumarin; Minimum inhibitory concentration; Single crystal; Staphylococcus aureus