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首页> 外文期刊>Journal of Medicinal Chemistry >Discovery of a Teraryl Oxazolidinone Compound (S)-N-((3-(3-Fluoro-4-(4-(pyridin-2-yl)-1H-pyrazol-1-yl)phenyl)-2-oxooxazolidin-5-yl)-methyl)acetamide Phosphate as a Novel Antimicrobial Agent with Enhanced Safety Profile and Efficacies
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Discovery of a Teraryl Oxazolidinone Compound (S)-N-((3-(3-Fluoro-4-(4-(pyridin-2-yl)-1H-pyrazol-1-yl)phenyl)-2-oxooxazolidin-5-yl)-methyl)acetamide Phosphate as a Novel Antimicrobial Agent with Enhanced Safety Profile and Efficacies

机译：发现芳基恶唑烷酮化合物（S）-N-（（3-（3-氟-4-（4-（吡啶-2-基）-1H-吡唑-1-基）苯基）-2-氧杂唑烷酮-5 -基）-甲基）乙酰胺磷酸酯作为一种新型抗菌剂，具有增强的安全性和功效

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摘要

A series of novel teraryl oxazolidinone compounds was designed, synthesized, and evaluated for their antimicrobial activity and toxicities. The compounds with aromatic N-heterocyclic substituents at the 4-position of pyrazolyl ring showed better antibacterial activity against the tested bacteria than other compounds with different patterns of substitution. Among all potent compounds, 10f exhibited promising safety profile in MTT assays and in hERG K+ channel inhibition test. Furthermore, its phosphate was found to be highly soluble in water (47.1 mg/mL), which is beneficial for the subsequent in vivo test. In MRSA systemic infection mice models, 10f phosphate exerted significantly improved survival protection compared with linezolid. The compound also demonstrated high oral bioavailability (F = 99.1%). Moreover, from the results of in vivo toxicology experiments, 10f phosphate would be predicted to have less bone marrow suppression.
机译：设计，合成并评估了一系列新型的芳基恶唑烷酮化合物的抗菌活性和毒性。在吡唑基环的4-位带有芳族N-杂环取代基的化合物比其他具有不同取代方式的化合物对被测细菌表现出更好的抗菌活性。在所有有效化合物中，10f在MTT分析和hERG K +通道抑制试验中显示出有希望的安全性。此外，发现其磷酸盐高度溶于水（47.1 mg / mL），这对于随后的体内测试是有益的。在MRSA全身感染小鼠模型中，与利奈唑胺相比，10f磷酸盐具有明显改善的生存保护。该化合物还具有较高的口服生物利用度（F = 99.1％）。此外，从体内毒理学实验的结果来看，预计10f磷酸盐的骨髓抑制作用较小。

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