| 摘要 |
透过甲醯化胜肽，比如N-甲醯甲硫氨醯亮氨醯苯丙氨酸(fMLF)与甲醯化胜肽受体第1型(FPR1)结合，可活化嗜中性白血球；上述反应可以发展成治疗无菌性或败血性发炎疾病的治疗标的。如式一之双胜肽类衍生物，其中R1、R4分别选自氢基(hydrogen atom)、羟基(hydroxyl group)、C1-C4烷基取代之羟基、C1-C4烷氧基(alkoxyl)、羧酸基团(carboxylic acids group)，醯胺基团含有C1-C4烷基(alkyl)氰基之取代、或C1-C4烷基或C1-C4烷氧基之取代，酯基团含有C1-C4烷基(alkyl)之取代或苯环上含有C1-C4烷基(alkyl)取代之苯醯基团(benzoyl group)其中之一；R2、R3分别选自氢基、羟基、苯基(phenyl group)、吡啶(pyridinyl)、羧酸基团(carboxylic acids group)，或是含有C1-C4烷氧基之酯基团，或是在苯环上含有羟基、卤素、C1-C4烷氧基(alkoxyl)或C1-C4烷基(alkyl)取代之苯醯基团(benzoyl group)。此外，式一所列的双胜肽类衍生物其两对掌中心分别为S与R构型。;Binding of fomyl peptide receptor 1 (FPR1) byN-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-C4alkyl, C1-C4alkoxyl 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-C4alkoxyl substitute on the ester group, and a hydroxyl group, halogen group, C1-C4alkoxyl group, C1-C4alkyl group substitute on the aromatic ring of benzoyl group. Additionally, the configurations of two amino acids areSandRconfigurations, respectively. |
