The history of the tetracyclines
The history of the tetracyclines
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DOI：
10.1111/j.1749-6632.2011.06354.x
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发表时间：
2011-01-01
期刊：
影响因子：
--
通讯作者：
Levy, Stuart B.
中科院分区：
文献类型：
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作者：
Nelson, Mark L.;Levy, Stuart B.
四环素类药物的历史涉及到60多年来数千名专门研究人员、科学家、临床医生和企业高管的集体贡献。四环素是放线菌和土壤细菌的天然产物，于1948年首次在科学文献中报道。它们以其广谱抗菌活性而闻名，并在20世纪40年代末至50年代初开始商业化并取得临床成功。第二代半合成类似物和最近的第三代化合物显示四环素支架向具有增加的效力以及对四环素耐药性细菌的功效的衍生物的持续演变，具有改善的药代动力学和化学性质。它们对广谱微生物病原体的生物活性及其在炎症、神经变性和其他生物系统的哺乳动物模型中的用途表明四环素类将继续是感染性疾病的成功治疗剂，并作为对抗基于炎症的哺乳动物细胞疾病的潜在治疗剂。
The history of the tetracyclines involves the collective contributions of thousands of dedicated researchers, scientists, clinicians, and business executives over the course of more than 60 years. Discovered as natural products from actinomycetes soil bacteria, the tetracyclines were first reported in the scientific literature in 1948. They were noted for their broad spectrum antibacterial activity and were commercialized with clinical success beginning in the late 1940s to the early 1950s. The second-generation semisynthetic analogs and more recent third-generation compounds show the continued evolution of the tetracycline scaffold toward derivatives with increased potency as well as efficacy against tetracycline-resistant bacteria, with improved pharmacokinetic and chemical properties. Their biologic activity against a wide spectrum of microbial pathogens and their uses in mammalian models of inflammation, neurodegeneration, and other biological systems indicate that the tetracyclines will continue to be successful therapeutics in infectious diseases and as potential therapeutics against inflammation-based mammalian cell diseases.