TY - JOUR
T1 - Design and synthesis of new N-(fluorenyl-9-methoxycarbonyl) (Fmoc)-dipeptides as anti-inflammatory agents
AU - Yen, Chiao Ting
AU - Hwang, Tsong Long
AU - Wu, Yang Chang
AU - Hsieh, Pei Wen
PY - 2009/5
Y1 - 2009/5
N2 - 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 IC50 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.
AB - 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 IC50 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.
KW - Anti-inflammatory agents
KW - Aurantiamide derivatives
KW - Fmoc-based dipeptides
UR - http://www.scopus.com/inward/record.url?scp=62549132051&partnerID=8YFLogxK
U2 - 10.1016/j.ejmech.2008.11.008
DO - 10.1016/j.ejmech.2008.11.008
M3 - 文章
C2 - 19110343
AN - SCOPUS:62549132051
SN - 0223-5234
VL - 44
SP - 1933
EP - 1940
JO - European Journal of Medicinal Chemistry
JF - European Journal of Medicinal Chemistry
IS - 5
ER -