Synthesis of Biscoumarin and Dihydropyran Derivatives and Evaluation of Their Antibacterial Activity

Molecules

Jing Li²  Chang-Wei Lv⁴  Xiao-Jun Li²  Di Qu¹  Zheng Hou¹  Min Jia¹  Xiao-Xing Luo¹  Xia Li³  Ming-Kai Li¹ 

[1] Department of Pharmacology, School of Pharmacy, the Fourth Military Medical University, Xi’an 710032, China; E-Mails:;School of Chemical Engineering, Xi’an University, Xi’an 710065, China; E-Mails:;Department of Neurosurgery, Xijing Hospital, the Fourth Military Medical University, Xi’an 710032, China;Department of Orthopaedics, Xijing Hospital, the Fourth Military Medical University, Xi’an 710032, China; E-Mail:

关键词: biscoumarins;    dihydropyran;    S. aureus;    S. epidermidis;   

DOI  :  10.3390/molecules200917469

来源: mdpi

【 摘 要 】

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.

【 授权许可】

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© 2015 by the authors; licensee MDPI, Basel, Switzerland.