Department of Medicinal Chemistry, New Drug Discovery Research, Ranbaxy Laboratories Limited, R&D III, Plot No. 20, Sector-18, Udyog Vihar Industrial Area, Gurgaon 122001, India.
Bioorg Med Chem Lett. 2011 Sep 15;21(18):5266-9. doi: 10.1016/j.bmcl.2011.07.034. Epub 2011 Jul 19.
The synthesis and antibacterial activity of 1,2,4-triazolo[4,3-a]pyrimidine oxazolidinones is reported. Compound 3e with a 2,4-disubstituted thiophene ring was found to be a potent inhibitor of Gram-positive pathogens and was 4-16-fold more potent than Linezolid.
报告了 1,2,4-三唑并[4,3-a]嘧啶恶唑烷酮的合成及抗菌活性。发现具有 2,4-二取代噻吩环的化合物 3e 是革兰氏阳性病原体的有效抑制剂,其活性比利奈唑胺强 4-16 倍。