Zhu Bin, Marinelli Brett A, Goldschmidt Raul, Foleno Barbara D, Hilliard Jamese J, Bush Karen, Macielag Mark J
Research & Early Development, Johnson & Johnson Pharmaceutical Research & Development, L.L.C., Welsh and McKean Roads, Spring House, PA 19477, USA.
Bioorg Med Chem Lett. 2009 Sep 1;19(17):4933-6. doi: 10.1016/j.bmcl.2009.07.087. Epub 2009 Jul 22.
A novel series of 7-(1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazin-7-yl) quinolones has been designed and synthesized in which the heterocyclic side chain is attached to the quinolone core through a carbon-carbon linkage. The antibacterial activity of the compounds was determined against a panel of Gram-positive and Gram-negative pathogens. Compounds 1b and 1e, bearing an 8-methoxy group as well as unsubstituted and (3S)-methyl substituted 1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazin-7-yl side chains, respectively, demonstrated notable activity against ciprofloxacin-resistant clinical isolates of Streptococcus pneumoniae.
设计并合成了一系列新型的7-(1,2,3,4-四氢吡咯并[1,2-a]吡嗪-7-基)喹诺酮类化合物，其中杂环侧链通过碳-碳键连接到喹诺酮核心上。测定了这些化合物对一组革兰氏阳性和革兰氏阴性病原体的抗菌活性。分别带有8-甲氧基以及未取代和(3S)-甲基取代的1,2,3,4-四氢吡咯并[1,2-a]吡嗪-7-基侧链的化合物1b和1e，对耐环丙沙星的肺炎链球菌临床分离株表现出显著活性。
