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.
复制标题
DOI:
10.1016/j.bmc.2009.04.038
复制
发表时间:
2009-06-01
影响因子:
3.5
通讯作者:
Xu W
中科院分区:
文献类型:
--
作者:
Yang K;Wang Q;Su L;Fang H;Wang X;Gong J;Wang B;Xu W
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).
登录
查看更多内容
DOI:
10.1073/pnas.0606167103
发表时间:
2006-09-05
影响因子:
11.1
作者:
Addlagatta, Anthony;Gay, Leslie;Matthews, Brian W.
通讯作者:
Matthews, Brian W.
影响因子:
3.5
作者:
Tu, GuoGang;Li, ShaoHua;Xu, Wen Fang
通讯作者:
Xu, Wen Fang
影响因子:
3.5
作者:
Flipo, Marion;Beghyn, Terence;Deprez-Poulain, Rebecca F.
通讯作者:
Deprez-Poulain, Rebecca F.
影响因子:
4.8
作者:
Ito, Kiyoshi;Nakajima, Yoshitaka;Yoshimoto, Tadashi
通讯作者:
Yoshimoto, Tadashi
影响因子:
2.7
作者:
Li, Qianbin;Fang, Hao;Xu, Wenfang
通讯作者:
Xu, Wenfang