Design and synthesis of novel chloramphenicol amine derivatives as potent aminopeptidase N (APN/CD13) inhibitors |
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| Authors: | Kanghui Yang Qiang Wang Li Su Hao Fang Xuejian Wang Jianzhi Gong Binghe Wang Wenfang Xu |
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| Institution: | 1. Department of Medicinal Chemistry, School of Pharmacy, Shandong University, 44 West Culture Road, Ji’nan, Shandong 250012, China;2. Department of Chemistry, Georgia State University, Atlanta, 30303, USA |
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| 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 (IC50 = 7.1 μM), possess similar APN inhibitory activity compared with Bestatin (IC50 = 3.0 μM). |
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