Citation: Jin Pei Zhou, Yi Wei Ding, Hui Bin Zhang, Lian Xu, Yue Dai. Synthesis and anti-inflammatory activity of imidazo [1,2-a] pyrimidine derivatives[J]. Chinese Chemical Letters, ;2008, 19(6): 669-672. doi: 10.1016/j.cclet.2008.04.020 shu

Synthesis and anti-inflammatory activity of imidazo [1,2-a] pyrimidine derivatives

a Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China;
b Department of Medicinal Chemistry, Jiangsu Staff Medical University, Nanjing 210029, China;
c National Drug Screening Center, China Pharmaceutical University, Nanjing 210038, China

Received Date: 3 January 2008

Fund Project: This research was supported by the National Natural Science Foundation of China (No. 30472083).

A series of imidazo [1,2-a] pyrimidine derivatives substituted adjacently with two aryls at positions 2 and 3 were designed and synthesized in order to improve their anti-inflammatory activities. Biological tests suggested that these compounds have antiinflammatory activities with COX-2 selectivity to some extent.
- Imidazo [1,2-a] pyrimidine,
- Cyclooxygenase-2,
- Anti-inflammatory,
- Synthesis
1. [1]
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2. [2]
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3. [3]
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