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

Design and synthesis of novel chloramphenicol amine derivatives as potent aminopeptidase N (APN/CD13) inhibitors.
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DOI:
10.1016/j.bmc.2009.04.038
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发表时间:
2009-06-01
影响因子:
3.5
通讯作者:
Xu W
Xu W
中科院分区:
医学3区
文献类型:
--
作者:
Yang K;Wang Q;Su L;Fang H;Wang X;Gong J;Wang B;Xu W

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The compound 13b was built and docked into the active site of APN (PDB code: 2DQM) using sybyl7.0. The docking result of 13b is showed by Ligplot. 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 μM), possess similar APN inhibitory activity compared with Bestatin (IC50 = 3.0 μM).
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