1,3-噁唑杂合体抗金黄色葡萄球菌活性研究

Recent Advances in the Application of 1,3-oxazole Hybrids to Fight against Staphylococcus aureus

金黄色葡萄球菌,广泛存在于自然界中,是一种人兽共患病原菌,可导致多种疾病甚至死亡,严重威胁人类健康。20世纪40年代青霉素问世后,金黄色葡萄球菌引起的感染性疾病曾一度得到了有效控制。但随着抗菌药的长期、广泛使用,耐药金黄色葡萄球菌不断涌现并迅速肆虐全球。据统计,每年全球感染耐药性金黄色葡萄球菌的人数高达数百万,其中约三分之一患者因此失去生命。开发新型抗菌药是克服耐药性的主要手段之一,而杂环化合物在抗菌新药的研发中占据主导地位。其中,1,3-噁唑类化合物具有潜在的抗菌活性,值得进一步研究。本文将归纳自2011年以来所发展的具有抗金黄色葡萄球菌活性的1,3-噁唑杂合体,并探讨其构-效关系,以期为今后发现新型药物候选物提供理论支持。

Staphylococcus aureus (S.aureus),exists widely in nature,is a zoonotic pathogen,which can lead to diverse diseases even death.Thus,S.aureus poses a great threath to human health.The infectious diseases caused by S.aureus were once effectively controlled since the advent of penicillin in 1940s.However,with the long-term and extensive application of antibiotics,drug-resistant S.aureus strains are constantly emerging and rapidly spread all over the world.It is estimated that millions of people infect drug-resistant S.aureus annually,and around one third of the patients die from the infection.The development of new antibacterial agents is one of the main means to overcome drug resistance,and heterocycles play a vital role in the discovery of novel antibacterial agents.Among them,1,3-oxazoles have potential antibacterial activity and are worthy of further study.In this review,the 1,3-oxazole hybrids with anti-S.aureus activity developed since 2011 is summarized,and their structure-activity relationships are discussed,to provide theoretical support for the discovery of new drug candidates in the future.