Varshney Vandana, Mishra Nripendra N, Shukla Praveen K, Sahu Devi P
Medicinal & Process Chemistry Division, Central Drug Research Institute, Lucknow 226 001, India.
Bioorg Med Chem Lett. 2009 Jul 1;19(13):3573-6. doi: 10.1016/j.bmcl.2009.04.133. Epub 2009 May 3.
A series of (5S) N-(3-{3-fluoro-4-[4-(3-aryl-4,5-dihydro-isoxazole-5-carbonyl)-piperazin-1-yl]-phenyl}-2-oxo-oxazolidin-5-ylmethyl)-acetamide(6a-o) were synthesized and their in vitro antibacterial activity against various resistant Gram-positive and Gram-negative bacteria were evaluated. Most of the synthesized compounds showed 2 to 10 fold lower MIC values compared to linezolid against Staphylococcus aureusATCC 25923, ATCC 70069, ATCC 29213,Bacillus cereusMTCC 430,Enterococcus faecalisMTCC439,Klebsiella pneumoniaeATCC 27736, and Streptococcus pyogens.
合成了一系列(5S)-N-(3-{3-氟-4-[4-(3-芳基-4,5-二氢异恶唑-5-羰基)-哌嗪-1-基]-苯基}-2-氧代-恶唑烷-5-基甲基)-乙酰胺(6a-o)，并评估了它们对各种耐药革兰氏阳性菌和革兰氏阴性菌的体外抗菌活性。与利奈唑胺相比，大多数合成化合物对金黄色葡萄球菌ATCC 25923、ATCC 70069、ATCC 29213、蜡样芽孢杆菌MTCC 430、粪肠球菌MTCC439、肺炎克雷伯菌ATCC 27736和化脓性链球菌的最低抑菌浓度值低2至10倍。
