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.

二十四个新的二肽类似物（1 - 24）乙酸乙酯aurantiamide的设计，合成，并测定响应于的fMLP / CB超氧阴离子的产生和弹性蛋白酶释放的影响人类嗜中性粒细胞。其中，7 ñ - （芴基-9-甲氧羰基）羰基（Fmoc）-dipeptides（6，9，12，14，17，18和20）显示了强的抑制效果。化合物9和18对人嗜中性白细胞弹性蛋白酶的释放表现出最强的选择性，IC ₅₀在该抗炎性检测中，其分别为0.8±0.1和1.7±0.6μM的浓度，且效力比阳性对照苯基甲基磺酰氟（PMSF）高130倍。可以开发这两种化合物作为新的抗炎药。