Chinese Journal of Applied Chemistry ›› 2011, Vol. 28 ›› Issue (02): 209-213.DOI: 10.3724/SP.J.1095.2011.00248

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

JIANG Yin-Zhi*, ZHOU Jun, LIANG Da-Wei, JIANG Ling-Bo, LIU Zheng-Jiang   

  1. (Department of Chemistry,Zhejiang Science-Technique University,Hangzhou 310018)
  • Received:2010-04-29 Revised:2010-07-01 Published:2011-02-10 Online:2011-02-10


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.

Key words: Pyrimidine, Synthesis, EcMetAP, CXCR4, Structure-Activity relationship

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