Ebner David C, Culhane Jeffrey C, Winkelman Tyler N, Haustein Mitchell D, Ditty Jayna L, Ippoliti J Thomas
Department of Chemistry, University of St. Thomas, St. Paul, MN 55105, USA.
Bioorg Med Chem. 2008 Mar 1;16(5):2651-6. doi: 10.1016/j.bmc.2007.11.040. Epub 2007 Nov 19.
The oxazolidinone class of antimicrobials represents a promising advance in the fight against resistant Gram-positive bacterial infections. Four novel oxazolidinone antimicrobial compounds, each containing a benzodioxin ring system, have been prepared. The general synthesis of each compound begins with the construction of a benzodioxin ring system containing a nitro substituent that ultimately becomes the nitrogen of the oxazolidinone ring. Three of the compounds utilize high yielding 'click chemistry' in their final step. The antimicrobial activities of the new oxazolidinones have been measured and the MIC against Staphylococcus aureus for one of the antimicrobials was determined to be 2-3 microg/mL, which is comparable to the well-known oxazolidinone, linezolid.
恶唑烷酮类抗菌药物是对抗革兰氏阳性菌耐药感染的一项有前景的进展。现已制备出四种新型恶唑烷酮抗菌化合物，每种都含有苯并二恶英环系。每种化合物的一般合成过程始于构建一个含有硝基取代基的苯并二恶英环系，该硝基取代基最终成为恶唑烷酮环的氮原子。其中三种化合物在其最后一步采用了高产率的“点击化学”。已对新型恶唑烷酮的抗菌活性进行了测定，其中一种抗菌药物对金黄色葡萄球菌的最低抑菌浓度（MIC）测定为2 - 3微克/毫升，这与著名的恶唑烷酮类药物利奈唑胺相当。
