Mingxiao Wang

Publications (3)9.81 Total impact

• Article: Design, synthesis and antiviral activity of novel pyridazines.

  Ziwen Wang, Mingxiao Wang, Xue Yao, Yue Li, Juan Tan, Lizhong Wang, Wentao Qiao, Yunqi Geng, Yuxiu Liu, Qingmin Wang
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  ABSTRACT: A series of pyridazines were prepared and evaluated for their anti-HIV activity. The new synthetic route involving a novel rearrangement reaction provided a practical method for the preparation of 5-hydroxypyridazines. The primary bioassay results indicated that most of the pyridazines possess anti-HIV activity. It ought to been mentioned that the rearranged compounds 35 and 39 exhibited relatively higher HIV inhibitory effect. Most of the synthesized compounds were also found to possess good anti-TMV activity, of which compound 9 showed similar in vivo anti-TMV activity to commercial plant virucide Ribavirin. This work provides a new and efficient approach to evolve novel multi-functional antiviral agents by rational integration and optimization of previously reported antiviral agents.
  European journal of medicinal chemistry 04/2012; 54:33-41. · 3.27 Impact Factor
• Article: Design, synthesis and antiviral activity of novel quinazolinones.

  Ziwen Wang, Mingxiao Wang, Xue Yao, Yue Li, Juan Tan, Lizhong Wang, Wentao Qiao, Yunqi Geng, Yuxiu Liu, Qingmin Wang
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  ABSTRACT: HIV-1 integrase (IN) is a validated therapeutic target for antiviral drug design. However, the emergence of viral strains resistant to clinically studied IN inhibitors demands the discovery of novel inhibitors that are structurally as well as mechanistically different. Herein, a series of quinazolinones were designed and synthesized as novel HIV-1 inhibitors. The new synthetic route provides a practical method for the preparation of 5-hydroxy quinazolinones. Primary bioassay results indicated that most of the quinazolinones possess anti-HIV activity, especially for compound 11b with 77.5% inhibition rate at 10 μM emerged as a new active lead. Most of the synthesized compounds were also found to exhibit good anti-TMV activity, of which compo und 9a showed similar in vivo anti-TMV activity to commercial plant virucide Ribavirin. This work provides a new and efficient approach to evolve novel multi-functional antiviral agents by rational integration and optimization of previously reported antiviral agents.
  European journal of medicinal chemistry 04/2012; 53:275-82. · 3.27 Impact Factor
• Article: Hydroxyl may not be indispensable for raltegravir: Design, synthesis and SAR Studies of raltegravir derivatives as HIV-1 inhibitors.

  Ziwen Wang, Mingxiao Wang, Xue Yao, Yue Li, Wentao Qiao, Yunqi Geng, Yuxiu Liu, Qingmin Wang
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  ABSTRACT: A series of raltegravir derivatives 20-42 were prepared and systematically evaluated for their anti-HIV activity. The bioassay results showed that most of the compounds possess good to excellent anti-HIV activity. Especially, compounds 25 and 35 with subpicomole IC(50) values seemed to be the most potent anti-HIV agents among all of the reported synthesized compounds. These compounds may therefore be considered as new potent anti-HIV agents. The 5-hydroxyl modification of raltegravir derivatives significantly increased the anti-HIV activity, which indicates that the hydroxyl may not be indispensable for raltegravir. The introducing of acyl at 5-position of raltegravir derivatives is favorable for antiviral activity. In addition, a high-throughput cell-based assay method with pseudotyped virus stocks was developed and used to identify HIV inhibitors.
  European journal of medicinal chemistry 02/2012; 50:361-9. · 3.27 Impact Factor