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随着细菌耐药现象的日益严重,从天然产物中寻找抗菌机制独特的先导化合物已成为新型抗菌药物开发的重要手段。因此,先前未被开发作为人类使用的兽用抗菌药物也得到了重新评估。妙林类抗生素是由担子菌产生的一种三环二萜类化合物,主要作用于50S核糖体亚基,通过抑制肽基转移酶的活性而使细菌的蛋白质合成受阻,其中主要代表药物泰妙菌素和沃尼妙林作为兽用抗生素已被广泛使用。新近衍生物retapamulin作为人用抗生素成功上市,实现了妙林类化合物从兽用抗生素到人用抗生素的飞跃,掀起了新型人用妙林类化合物研究开发的浪潮。文中着重就2004-2008年人用妙林类抗生素的开发以及专利的相关最新进展进行简要综述。
With the increasing resistance of bacteria, looking for the lead compound with unique antibacterial mechanism from natural products has become an important means to develop new antibacterial drugs. Therefore, veterinary antimicrobials that have not previously been developed for human use have also been re-evaluated. Miao Lin antibiotics is a tricyclic diterpenoid produced by the basidiomycetes, the main role in the 50S ribosomal subunits, by inhibiting the activity of peptidyl transferases and bacterial protein synthesis blocked, which mainly represents the drug Miao Mycin and Woney Miaolin as veterinary antibiotics have been widely used. The recent success of the retapamulin derivative as a human antibiotic marketed a quantum leap forward in animal-derived antibiotics to human antibiotics and set off a wave of research and development for the new type of human felines. This article focuses on the 2004-2008 people with wonderful forest antibiotics development and patents related to the latest progress made a brief review.