Abstract
In an attempt to find a new class antibacterial agents, a series of biscoumarins (1–4) and dihydropyrans (5–13) were successfully prepared. The molecular structures of four representative compounds, that is, 4, 5, 8 and 12 were confirmed by single crystal X-ray diffraction study. These synthesized compounds were screened for their antibacterial activity in vitro against Staphylococcus aureus (S. aureus ATCC 29213), methicillin-resistant S. aureus (MRSA XJ 75302), vancomycin-intermediate S. aureus (Mu50 ATCC 700699), USA 300 (Los Angeles County clone, LAC), Staphylococcus epidermidis (S. epidermidis ATCC 14990), methicillin-resistant S. epidermidis (MRSE XJ 75284) and Escherichia coli (E. coli ATCC 25922). Additionally, there are two classical intramolecular O–H···O hydrogen bonds (HBs) in biscoumarins 1–4 and the corresponding HB energies were further performed with the density functional theory (DFT) [B3LYP/6-31G*] method.
Highlights
Staphylococcus aureus (S. aureus) is a common pathogen causing serious hospital infections, community acquired infections and is the pathogen with the highest drug resistant incidence.There are still no specific and selective antibacterial agents to kill Methicillin-resistant S. aureus (MRSA) (Methicillin-resistantS. aureus), which leads to a high death rate of patients [1]
To further explore the safety of the possible development, we investigated the cytotoxicity of compounds 3 and 4 to human umbilical vein endothelial cells (HUVECs) and human embryonic cardiomyocyte cell line CCC-HHM-2 (HHHM-2) in vitro
Methicillin-resistant S. aureus (MRSA) and is the cause of major outbreaks and epidemics in hospitalized patients because of the emergence, spread, and rapid evolution of resistance genes developing among pathogens
Summary
Staphylococcus aureus (S. aureus) is a common pathogen causing serious hospital infections, community acquired infections and is the pathogen with the highest drug resistant incidence.There are still no specific and selective antibacterial agents to kill MRSA (Methicillin-resistantS. aureus), which leads to a high death rate of patients [1]. Staphylococcus aureus (S. aureus) is a common pathogen causing serious hospital infections, community acquired infections and is the pathogen with the highest drug resistant incidence. There are still no specific and selective antibacterial agents to kill MRSA Resistance to antibacterial drugs has been relentlessly increasing over the past two decades, along with a noticeable decrease in the development of new drugs for infections [2]. Few candidate drugs that offer benefits over existing drugs are available, and few drugs that will treat infections due to the so-called “ESKAPE” pathogens (Enterococcus faecium, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, and Enterobacter spp.) are being developed [3]. Pathogens including MRSA and to develop 10 new effective antimicrobial drugs to treat the infections caused by these pathogens by 2020 [4]. It is evident and urgent to seek a new defending strategy against MRSA
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