2. Academic Validation
  3. Design and synthesis of new N-(fluorenyl-9-methoxycarbonyl) (Fmoc)-dipeptides as anti-inflammatory agents

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

  • Eur J Med Chem. 2009 May;44(5):1933-40. doi: 10.1016/j.ejmech.2008.11.008.
Chiao-Ting Yen 1,  Tsong-Long Hwang,  Yang-Chang Wu,  Pei-Wen Hsieh
Affiliations

Affiliation

  • 1 Graduate Institute of Natural Products, Kaohsiung Medical University, Kaohsiung 807, Taiwan.
PMID: 19110343 DOI: 10.1016/j.ejmech.2008.11.008
Abstract

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+/-0.6muM, 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.

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