Ellsworth Edmund L, Tran Tuan P, Showalter H D Hollis, Sanchez Joseph P, Watson Brian M, Stier Michael A, Domagala John M, Gracheck Stephen J, Joannides E Themis, Shapiro Martin A, Dunham Steve A, Hanna Debra L, Huband Michael D, Gage Jeffrey W, Bronstein Joel C, Liu Jia Yeu, Nguyen Dai Q, Singh Rajeshwar
Pfizer Global Research and Development, Michigan Laboratories, 2800 Plymouth Road, Ann Arbor, MI 48105, USA.
J Med Chem. 2006 Nov 2;49(22):6435-8. doi: 10.1021/jm060505l.
The 3-aminoquinzolinediones represent a new series of antibacterial agents structurally related to the fluoroquinolones. They are inhibitors of bacterial gyrase and topoisomerase IV and demonstrate clinically useful antibacterial activity against fastidious Gram-negative and Gram-positive organisms, including multidrug- and fluoroquinolone-resistant organisms. These agents also demonstrate in vivo efficacy in murine systemic infection models.
3-氨基喹唑啉二酮代表了一系列结构上与氟喹诺酮类相关的新型抗菌剂。它们是细菌gyrase和拓扑异构酶IV的抑制剂，对苛求革兰氏阴性和革兰氏阳性菌，包括耐多药和耐氟喹诺酮菌，具有临床上有用的抗菌活性。这些药物在小鼠全身感染模型中也显示出体内疗效。
