7-(3-氨基-6,7-二氢-2-甲基-2H-吡唑并[4,3-c]吡啶-5(4H)-基)氟喹诺酮衍生物的合成及体外抗菌活性。
Synthesis and in vitro antibacterial activity of 7-(3-amino-6,7-dihydro-2-methyl-2H-pyrazolo[4,3-c] pyridin-5(4H)-yl)fluoroquinolone derivatives.
机构信息
Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
出版信息
Molecules. 2011 Mar 22;16(3):2626-35. doi: 10.3390/molecules16032626.
A series of novel 7-(3-amino-6,7-dihydro-2-methyl-2H-pyrazolo[4,3-c]pyridin- 5(4H)-yl)fluoroquinolone derivatives were designed, synthesized and characterized by 1H-NMR, MS and HRMS. These fluoroquinolones were evaluated for their in vitro antibacterial activity against representative Gram-positive and Gram-negative strains. Results reveal that most of the target compounds exhibit good growth inhibitory potency against methicillin-resistant Staphylococcus epidermidis (MRSE) (MIC: 0.25-4 μg/mL) and Streptococcus pneumoniae (MIC: 0.25-1 μg/mL). In addition, compound 8f is 8-128 fold more potent than the reference drugs gemifloxacin (GM), moxifloxacin (MX), ciprofloxacin (CP) and levofloxacin (LV) against methicillin-resistant Staphylococcus aureus 10-05 and Streptococcus hemolyticus 1002 and 2-64 fold more active against methicillin-sensitive Staphylococcus aureus 10-03 and 10-04.
设计、合成并通过 1H-NMR、MS 和 HRMS 对一系列新型 7-(3-氨基-6,7-二氢-2-甲基-2H-吡唑并[4,3-c]吡啶-5(4H)-基)氟喹诺酮衍生物进行了表征。通过评估这些氟喹诺酮类化合物对代表性革兰氏阳性和革兰氏阴性菌株的体外抗菌活性。结果表明，大多数目标化合物对耐甲氧西林表皮葡萄球菌（MRSE）（MIC：0.25-4 μg/mL）和肺炎链球菌（MIC：0.25-1 μg/mL）具有良好的生长抑制作用。此外，化合物 8f 对耐甲氧西林金黄色葡萄球菌 10-05 和溶血性链球菌 1002 的活性比参考药物加替沙星（GM）、莫西沙星（MX）、环丙沙星（CP）和左氧氟沙星（LV）高 8-128 倍，对甲氧西林敏感金黄色葡萄球菌 10-03 和 10-04 的活性高 2-64 倍。
Zotero 插件