European Journal of Medicinal Chemistry 2009-01-01

Design and synthesis of newN-(fluorenyl-9-methoxycarbonyl) (Fmoc)-dipeptides as anti-inflammatory agents

Chiao-Ting Yen, Tsong-Long Hwang, Yang-Chang Wu, Pei-Wen Hsieh

文献索引：Eur. J. Med. Chem. 44 , 1933-40, (2009)

全文：HTML全文

摘要

Twenty-four new dipeptide analogs ( 1– 24) of aurantiamide acetate were designed, synthesized, and assayed for effects on superoxide anion generation and elastase release by human neutrophils in response to fMLP/CB. Among them, seven N-(fluorenyl-9-methoxycarbonyl) (Fmoc)-dipeptides ( 6, 9, 12, 14, 17, 18 and 20) showed potent inhibitory effects. Compounds 9 and 18 showed the most selective effects against human neutrophil elastase release, with IC 50 values of 0.8 ± 0.1 and 1.7 ± 0.6 μM, respectively, and were 130-fold more potent than phenylmethylsulfonyl fluoride (PMSF), the positive control, in this anti-inflammatory assay. These two compounds could be developed as new lead anti-inflammatory agents.

相关化合物

  • 苄磺酰氟
  • Fmoc-L-酪氨酸
  • Fmoc-O-叔丁基-L-...
  • FMOC-L-色氨酸
  • Fmoc-L-异亮氨酸
  • Fmoc-L-缬氨酸
  • Fmoc-L-苯丙氨酸

相关文献：

Immunomodulation by the Pseudomonas syringae HopZ type III effector family in Arabidopsis.

2014-01-01

[PLoS ONE 9(12) , e116152, (2014)]

Assembly and structure of Lys33-linked polyubiquitin reveals distinct conformations.

2015-04-15

[Biochem. J. 467(2) , 345-52, (2015)]

A survey of the interactome of Kaposi's sarcoma-associated herpesvirus ORF45 revealed its binding to viral ORF33 and cellular USP7, resulting in stabilization of ORF33 that is required for production of progeny viruses.

2015-05-01

[J. Virol. 89(9) , 4918-31, (2015)]

Analysis of cytochrome P450 CYP119 ligand-dependent conformational dynamics by two-dimensional NMR and X-ray crystallography.

2015-04-17

[J. Biol. Chem. 290(16) , 10000-17, (2015)]

An HD-domain phosphodiesterase mediates cooperative hydrolysis of c-di-AMP to affect bacterial growth and virulence.

2015-02-17

[Proc. Natl. Acad. Sci. U. S. A. 112(7) , E747-56, (2015)]

更多文献...