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

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 exhi...

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Detalles Bibliográficos
Autores principales: Yang, Kanghui, Wang, Qiang, Su, Li, Fang, Hao, Wang, Xuejian, Gong, Jianzhi, Wang, Binghe, Xu, Wenfang
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Published by Elsevier Ltd. 2009
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7172530/
https://www.ncbi.nlm.nih.gov/pubmed/19423354
http://dx.doi.org/10.1016/j.bmc.2009.04.038
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author Yang, Kanghui
Wang, Qiang
Su, Li
Fang, Hao
Wang, Xuejian
Gong, Jianzhi
Wang, Binghe
Xu, Wenfang
author_facet Yang, Kanghui
Wang, Qiang
Su, Li
Fang, Hao
Wang, Xuejian
Gong, Jianzhi
Wang, Binghe
Xu, Wenfang
author_sort Yang, Kanghui
collection PubMed
description 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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spelling pubmed-71725302020-04-22 Design and synthesis of novel chloramphenicol amine derivatives as potent aminopeptidase N (APN/CD13) inhibitors Yang, Kanghui Wang, Qiang Su, Li Fang, Hao Wang, Xuejian Gong, Jianzhi Wang, Binghe Xu, Wenfang Bioorg Med Chem Article 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). Published by Elsevier Ltd. 2009-06-01 2009-04-24 /pmc/articles/PMC7172530/ /pubmed/19423354 http://dx.doi.org/10.1016/j.bmc.2009.04.038 Text en Copyright © 2009 Published by Elsevier Ltd. Since January 2020 Elsevier has created a COVID-19 resource centre with free information in English and Mandarin on the novel coronavirus COVID-19. The COVID-19 resource centre is hosted on Elsevier Connect, the company's public news and information website. Elsevier hereby grants permission to make all its COVID-19-related research that is available on the COVID-19 resource centre - including this research content - immediately available in PubMed Central and other publicly funded repositories, such as the WHO COVID database with rights for unrestricted research re-use and analyses in any form or by any means with acknowledgement of the original source. These permissions are granted for free by Elsevier for as long as the COVID-19 resource centre remains active.
spellingShingle Article
Yang, Kanghui
Wang, Qiang
Su, Li
Fang, Hao
Wang, Xuejian
Gong, Jianzhi
Wang, Binghe
Xu, Wenfang
Design and synthesis of novel chloramphenicol amine derivatives as potent aminopeptidase N (APN/CD13) inhibitors
title Design and synthesis of novel chloramphenicol amine derivatives as potent aminopeptidase N (APN/CD13) inhibitors
title_full Design and synthesis of novel chloramphenicol amine derivatives as potent aminopeptidase N (APN/CD13) inhibitors
title_fullStr Design and synthesis of novel chloramphenicol amine derivatives as potent aminopeptidase N (APN/CD13) inhibitors
title_full_unstemmed Design and synthesis of novel chloramphenicol amine derivatives as potent aminopeptidase N (APN/CD13) inhibitors
title_short Design and synthesis of novel chloramphenicol amine derivatives as potent aminopeptidase N (APN/CD13) inhibitors
title_sort design and synthesis of novel chloramphenicol amine derivatives as potent aminopeptidase n (apn/cd13) inhibitors
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7172530/
https://www.ncbi.nlm.nih.gov/pubmed/19423354
http://dx.doi.org/10.1016/j.bmc.2009.04.038
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