Author: Yang, Kanghui; Wang, Qiang; Su, Li; Fang, Hao; Wang, Xuejian; Gong, Jianzhi; Wang, Binghe; Xu, Wenfang
Title: Design and synthesis of novel chloramphenicol amine derivatives as potent aminopeptidase N (APN/CD13) inhibitors Cord-id: 010lano6 Document date: 2009_6_1
ID: 010lano6
Snippet: 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 (IC(50) = 7.1 μM), possess similar APN inhibitory activity compared with Bestatin (IC(50) = 3.0 μM).
Document: 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 (IC(50) = 7.1 μM), possess similar APN inhibitory activity compared with Bestatin (IC(50) = 3.0 μM).
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