Yuanyuan Liu

Publications (3)11.21 Total impact

• Article: 3H-1,2,4-Dithiazol-3-one compounds as novel potential affordable antitubercular agents.

  Jianzhong Yang, Weiyi Pi, Li Xiong, Wei Ang, Tao Yang, Jun He, Yuanyuan Liu, Ying Chang, Weiwei Ye, Zhenling Wang, Youfu Luo, Yuquan Wei
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  ABSTRACT: Small molecules with oxathiazol-2-one moiety were recently reported as potent inhibitors of Mycobacterium bovis var. bacilli Calmette-Guérin (BCG), among which HT1171 was the most potent and selective proteasome inhibitor. Herein we synthesized a series of novel compounds by bioisosteric replacement of the oxathiazol-2-one ring with 3H-1,2,4-dithiazol-3-one, and also fifteen 1,3,4-oxathiazol-2-one molecules in order for potency comparison and structure-activity relationship elucidation since their antibacterial effects on the virulent strains were not evaluated before. All the compounds were assessed for antitubercular activities on the virulent H37Rv strain by a serial dilution method. Among the tested compounds, 3H-1,2,4-dithiazol-3-one compound 4n was found to be the most active with a lowest MIC(90) value of 1μg/mL. Furthermore, the cytotoxicities of all the compounds against normal human liver cell line L02 were determined by an MTT method. Compound 4n displayed a lower inhibitory ratio than HT1171 at the concentration of 100μM, indicating its better safety profile.
  Bioorganic & medicinal chemistry letters 01/2013; · 2.65 Impact Factor
• Article: Carrier-free nanoassemblies of a novel oxazolidinone compound FYL-67 display antimicrobial activity on methicillin-resistant Staphylococcus aureus.

  Changyang Gong, Tao Yang, Xiaoyan Yang, Yuanyuan Liu, Wei Ang, Jianying Tang, Weiyi Pi, Li Xiong, Ying Chang, Weiwei Ye, Zhenling Wang, Youfu Luo, Xia Zhao, Yuquan Wei
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  ABSTRACT: In this work, a novel oxazolidinone compound FYL-67 was synthesized, and the obtained FYL-67 could form nanoassemblies in aqueous solution by a self-assembly method without using any carrier, organic solvent, or surfactant. The prepared FYL-67 nanoassemblies had a particle size of 264.6 ± 4.3 nm. The FYL-67 nanoassemblies can be lyophilized into a powder form without any cryoprotector or excipient, and the re-dissolved FYL-67 nanoassemblies are stable and homogeneous. The in vitro release profile showed a significant difference between rapid release of free FYL-67 and much slower and sustained release of FYL-67 nanoassemblies. In vitro susceptibility tests were conducted in three strains of methicillin-susceptible Staphylococcus aureus (MSSA) and three strains of methicillin-resistant Staphylococcus aureus (MRSA), using linezolid as a positive control. FYL-67 nanoassemblies exhibited excellent in vitro activity, with a minimum inhibitory concentration (MIC) value of 0.5 μg mL(-1) against MRSA. In the in vitro post-antibiotic effect (PAE) evaluation, FYL-67 nanoassemblies showed a more powerful effect than linezolid. Besides, in vitro cytotoxicity tests indicated that FYL-67 nanoassemblies had a very low cytotoxicity on HEK293 cells and L02 cells. Furthermore, in both MSSA and MRSA systemic infection mouse models, FYL-67 nanoassemblies showed a lower ED(50) than linezolid. In a murine model of MRSA systemic infection, FYL-67 nanoassemblies displayed an ED(50) of less than 4.0 mg kg(-1), which is 2.3-fold better than that of linezolid. Our findings suggested that the FYL-67 nanoassemblies may be a potential drug candidate in MRSA therapy.
  Nanoscale 11/2012; · 5.91 Impact Factor
• Article: Design, synthesis and evaluation of novel molecules with a diphenyl ether nucleus as potential antitubercular agents.

  Yinghong Yang, Zhenling Wang, Jianzhong Yang, Tao Yang, Weiyi Pi, Wei Ang, Yanni Lin, Yuanyuan Liu, Zicheng Li, Youfu Luo, Yuquan Wei
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  ABSTRACT: A series of compounds with a diphenyl ether nucleus were synthesized by incorporating various amines into the diphenyl ether scaffold with an amide bond. Their antitubercular activities were evaluated against Mycobacterium tuberculosis H(37)Rv by a microdilution method, with MIC values ranging from 4 to 64μg/mL. Through structure-activity relationship studies, the two chlorine atoms at 3 and 4 positions in the phenyl ring of R(2) group were found to play a significant role in the antitubercular activity. The most potent compound 6c showed an MIC value of 4μg/mL and a good safety profile in HepG2 cell line by the MTT assay. Compound 6c was further found to be effective in a murine model of BCG infection, providing a good lead for subsequent optimization.
  Bioorganic & medicinal chemistry letters 12/2011; 22(2):954-7. · 2.65 Impact Factor