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Citation: JIANG Yinzhi, ZHOU Jun, LIANG Dawei, JIANG Lingbo, LIU Zhengjiang. Synthesis and Biological Activities of 4,6-Diaryl-2-aminopyrimidine Derivatives[J]. Chinese Journal of Applied Chemistry, ;2011, 28(2): 209-213. doi: 10.3724/SP.J.1095.2011.00248 shu

Synthesis and Biological Activities of 4,6-Diaryl-2-aminopyrimidine Derivatives

1.
Department of Chemistry, Zhejiang Science-Technique University, Hangzhou 310018

Corresponding author: JIANG Yinzhi,
Received Date: 29 April 2010
Available Online: 6 July 2010
Fund Project: 国家自然科学青年基金(20901067) (20901067)浙江省自然科学基金(Y4080342)资助项目 (Y4080342)

Five kinds of 4,6-diaryl-2-aminopyrimidine derivatives were synthesized and characterized by IR,MS and ¹H NMR.The Escherichia coli methionine aminopeptidase(EcMetAP) inhibit-activities and the CXCR4 receptor antogonists activities of the five compounds were determined.The results show that all the five compounds have the EcMetAP inhibit-activities,and they also have CXCR4 receptor antogonists activities except the compound 2.The structure-activity relationships were studied by the FieldTemplater and FieldAlign software through molecular field analysis.The results show that the pharmacophore could be 3-N atom and 4,6-bencycles used as the EcMetAP inhibitor,and the EcMetAP inhibit-activities could be increased by addition of electron-donating groups at 6-benzyl.It also shows that the pharmacophore could be 2-C atom and 4,6-bencycles used as the CXCR4 receptor antogonists.The CXCR4 receptor antogonists could be increased by addition of electron-donating substituent at 2-C.
- pyrimidine,
- synthesis,
- EcMetAP,
- CXCR4,
- structure-activity relationship
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