N-甲酰羟胺类肽去甲酰酶抑制剂的合成及抗菌活性

Synthesis and antibacterial activities of N-formylhydroxylamine derivatives as peptide deformylase inhibitors

目的设计合成N-甲酰羟胺类肽去甲酰酶抑制剂,初步评价其体外抗菌活性。方法以丙二酸二乙酯为起始原料,经多步反应合成目标化合物;采用对倍稀释法,测定目标化合物对金葡菌、表葡菌以及耐甲氧西林金葡菌、表葡菌的抑菌活性。结果与结论合成了14个未见文献报道的目标化合物,其结构经1H-NMR、MS确证。体外试验表明:目标化合物均表现出一定的抗菌活性。

Aim To design and synthesize a series of N-formylhydroxylamine derivatives as peptide deformylase inhibitors and evaluate their antibacterial activities in vitro primarily. Methods The target compounds were synthesized in several steps starting from diethyl malonate, and their antibacterial activities in vitro against Staphylococcus aureus, Staphylococcus epidermidis, methicillin-resistant Staphylococcus aureus, methicillin-resistant Staphylococcus epidermidis were examined respectively. Results and conclusion Fourteen novel compounds were synthesized and their structures were identified by ^1H-NMR and MS. The pharmaco-logical test show that all the target compounds have good antibacterial activities.