2. Academic Validation
  3. 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

  • Bioorg Med Chem. 2009 Jun 1;17(11):3810-7. doi: 10.1016/j.bmc.2009.04.038.
Kanghui Yang 1,  Qiang Wang,  Li Su,  Hao Fang,  Xuejian Wang,  Jianzhi Gong,  Binghe Wang,  Wenfang Xu
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, School of Pharmacy, Shandong University, 44 West Culture Road, Ji'nan, Shandong 250012, China.
PMID: 19423354 DOI: 10.1016/j.bmc.2009.04.038
Abstract

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 microM), possess similar APN inhibitory activity compared with Bestatin (IC(50)=3.0 microM).

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