A series of novel oxazolidinone antibacterials with diverse fused heteroaryl C-rings bearing hydrogen bond donor and hydrogen bond acceptor functionalities were designed and synthesized. The compound with benzoxazinone C-ring substructure (8c) exhibited superior activity compared to linezolid against a panel of Gram-positive and Gram-negative bacteria. Structural modifications at C5-side chain of 8c resulted in identification of several potent compounds (12a, 12b, 12g, and 12h). Selected compounds 8c and 12a showed very good microsomal stability and no CYP₄₅₀ liability, thus clearing preliminary safety hurdles. A docking model of 12a binding to 23S rRNA suggested that the increased potency of 12a is due to additional ligand–receptor interaction.

中文翻译：

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稠合杂环C环亚结构的恶唑烷酮的设计，合成及抗菌性能评价

设计并合成了一系列新颖的恶唑烷酮类抗菌剂，它们具有带有氢键供体和氢键受体功能的各种稠合杂芳基C环。与利奈唑胺相比，具有苯并恶嗪酮C环亚结构的化合物（8c）对一组革兰氏阳性和革兰氏阴性细菌表现出更高的活性。8c的C5侧链的结构修饰导致鉴定了几种有效的化合物（12a，12b，12g和12h）。选定的化合物8c和12a显示出非常好的微粒体稳定性，并且没有CYP ₄₅₀责任，从而消除了初步的安全障碍。的对接模型12A结合23S rRNA的建议的增强的效力12A是由于附加的配体-受体相互作用。