新型 1,2,4-三唑并[4,3-a]嘧啶恶唑烷酮类抗菌剂的合成及体外活性。
Synthesis and in vitro activity of novel 1,2,4-triazolo[4,3-a]pyrimidine oxazolidinone antibacterial agents.
机构信息
Department of Medicinal Chemistry, New Drug Discovery Research, Ranbaxy Laboratories Limited, R&D III, Plot No. 20, Sector-18, Udyog Vihar Industrial Area, Gurgaon 122 001, India.
出版信息
Bioorg Med Chem Lett. 2011 May 15;21(10):2887-9. doi: 10.1016/j.bmcl.2011.03.075. Epub 2011 Mar 29.
PMID:21507643
Abstract
The synthesis and antibacterial activity of 3-(4-([1,2,4]triazolo[4,3-a]pyrimidin-3-yl)phenyl)oxazolidin-2-ones is reported. Thiocarbonyl derivatives were found to be potent inhibitors of gram-positive pathogens and compound 4l was two to fourfold more potent than Linezolid.
摘要
报告了 3-(4-([1,2,4]三唑并[4,3-a]嘧啶-3-基)苯基)恶唑烷-2-酮的合成及抗菌活性。发现硫羰基衍生物是革兰氏阳性病原体的有效抑制剂，化合物 4l 的活性比利奈唑胺强 2 至 4 倍。
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