Binding of fomyl peptide receptor 1 (FPR1) by N-formyl peptides can induce neutrophil activation and may represent a new therapeutic target in either sterile or septic inflammation. In present application, a series of new dipeptide derivatives as shown general formula (I) is provided. Of these, each of R1 and R4 is one selected from a group consisting of hydrogen atom, hydroxyl group, C1-C4 alkyl, C1-C4 alkoxyl and glycin-nitrile amide group each of R2 and R3 is one selected from a group consisting of hydrogen atom, hydroxyl group, pyridinyl group, phenyl group, pyridinyl group, C1-C4 alkoxyl substitute on the ester group, and a hydroxyl group, halogen group, C1-C4 alkoxyl group, C1-C4 alkyl group substitute on the aromatic ring of benzoyl group. Additionally, the configurations of two amino acids are S and R configurations, respectively.透過甲醯化胜肽,比如N-甲醯甲硫氨醯亮氨醯苯丙氨酸(fMLF)與甲醯化胜肽受體第1型(FPR1)結合,可活化嗜中性白血球;上述反應可以發展成治療無菌性或敗血性發炎疾病的治療標的。如式一之雙胜肽類衍生物,其中R1、R4分別選自氫基(hydrogen atom)、羥基(hydroxyl group)、C1-C4烷基取代之羥基、C1-C4烷氧基(alkoxyl)、羧酸基團(carboxylic acids group),醯胺基團含有C1-C4烷基(alkyl)氰基之取代、或C1-C4烷基或C1-C4烷氧基之取代,酯基團含有C1-C4烷基(alkyl)之取代或苯環上含有C1-C4烷基(alkyl)取代之苯醯基團(benzoyl group)其中之一;R2、R3分別選自氫基、羥基、苯基(phenyl group)、吡啶(pyridinyl)、羧酸基團(carboxylic acids group),或是含有C1-C4烷氧基之酯基團,或是在苯環上含有羥基、鹵素、C1-C4烷氧基(alkoxyl)或C1-C4烷基(alkyl)取代之苯醯基團(benzoyl group)。此外,式一所列的雙胜肽類衍生物其兩對掌中心分別為S與R構型。
