Design and synthesis of novel chloramphenicol amine derivatives as potent aminopeptidase N(APN/CD13) inhibitors

作者：Yang, Kanghui; Wang, Qiang; Su, Li; Fang, Hao^*; Wang, Xuejian; Gong, Jianzhi; Wang, Binghe; Xu, Wenfang

来源：Bioorganic & Medicinal Chemistry, 2009, 17(11): 3810-3817.

DOI：10.1016/j.bmc.2009.04.038

• Synthesis
• Aminopeptidase N
• Chloramphenicol amine
• Inhibitor
• QSAR

Herein we report a series of novel chloramphenicol amine derivatives as aminopeptidase N (APN)/CD13 inhibitors. All compounds were synthesized starting from commercially available (1S, 2S)-2-amino-1-(4-nitrophenyl) propane-1,3-diol. The preliminary biological screening showed that some compounds exhibited potent inhibitory activity against APN. It should be noted that one compound, 13b (IC50 = 7.1 mu M), possess similar APN inhibitory activity compared with Bestatin (IC50 = 3.0 mu M).

• 出版日期2009-6-1
• 单位山东大学