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A series of imidazole derivatives were designed following rational drug design, and synthesized through microwave-assisted one-pot multicomponent reactions. These compounds are produced in large quantities, and are known to be tolerant toward a variety of substrates, thus providing target molecules in a single step within a short time. These compounds were further tested for their ability to inhibit indoleamine-2,3-dioxygenase 1 (IDO1). The most promising compound thus obtained is 4o, which displayed IC50 values of 0.82 μΜ. Further in vivo assessment indicated that 4o could reduce the kynurenine levels in plasma by 42.3% in 4 hr, indicating that the compound could act as a promising lead compound for further investigations.
Zhizheng Bai, and
Huidan Huang, and
Jianqiu Chen, and
Xiaoyun Zhang, and
Yimei Ding
March 2012,
Organic letters,
Zhizheng Bai, and
Huidan Huang, and
Jianqiu Chen, and
Xiaoyun Zhang, and
Yimei Ding
May 2011,
Molecular diversity,
Zhizheng Bai, and
Huidan Huang, and
Jianqiu Chen, and
Xiaoyun Zhang, and
Yimei Ding
April 2011,
Bioorganic & medicinal chemistry letters,
Zhizheng Bai, and
Huidan Huang, and
Jianqiu Chen, and
Xiaoyun Zhang, and
Yimei Ding
January 2011,
Bioorganic & medicinal chemistry letters,
Zhizheng Bai, and
Huidan Huang, and
Jianqiu Chen, and
Xiaoyun Zhang, and
Yimei Ding
November 2000,
Organic letters,
Zhizheng Bai, and
Huidan Huang, and
Jianqiu Chen, and
Xiaoyun Zhang, and
Yimei Ding
January 2003,
Molecular diversity,
Zhizheng Bai, and
Huidan Huang, and
Jianqiu Chen, and
Xiaoyun Zhang, and
Yimei Ding
May 2017,
Chemistry Central journal,
Zhizheng Bai, and
Huidan Huang, and
Jianqiu Chen, and
Xiaoyun Zhang, and
Yimei Ding
March 2013,
The Journal of organic chemistry,
Zhizheng Bai, and
Huidan Huang, and
Jianqiu Chen, and
Xiaoyun Zhang, and
Yimei Ding
January 2003,
Methods in enzymology,
Zhizheng Bai, and
Huidan Huang, and
Jianqiu Chen, and
Xiaoyun Zhang, and
Yimei Ding
August 2010,
Molecular diversity,
