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  • 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.

European journal of medicinal chemistry (2008-12-27)
Chiao-Ting Yen, Tsong-Long Hwang, Yang-Chang Wu, Pei-Wen Hsieh
RESUMO

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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Sigma-Aldrich
Phenylmethanesulfonyl fluoride, ≥98.5% (GC)
Sigma-Aldrich
Phenylmethanesulfonyl fluoride solution, ~0.1 M in ethanol (T)
Sigma-Aldrich
Fmoc-Phe-OH, 98%
Sigma-Aldrich
Fmoc-Tyr(tBu)-OH, ≥98.0% (HPLC)
Sigma-Aldrich
Fmoc-Val-OH, ≥98.0% (HPLC)
Sigma-Aldrich
Fmoc-Ile-OH, ≥98.0% (T)

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