Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, P.R. China.
Arch Pharm (Weinheim). 2011 Aug;344(8):523-9. doi: 10.1002/ardp.201000160. Epub 2011 Jun 8.
A series of novel 7-(3-aminopyrrolo[3,4-c]pyrazol-5(2H,4H,6H)-yl)-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid derivatives was designed, synthesized and characterized by (1)H-NMR, MS and HRMS. These fluoroquinolones were evaluated for their in-vitro antibacterial activity against representative Gram-positive and Gram-negative strains. Generally, all of the target compounds display rather weak potency against the tested Gram-negative strains, but most of them exhibit good potency in inhibiting the growth of S. aureus including methicillin-resistant Staphylococcus aureus (MRSA) and Staphylococcus epidermidis including methicillin-resistant S. epidermidis (MRSE) (MIC: 0.125-8 µg/mL). In particular, the compound 9g is 2 to 32 fold more potent than gemifloxacin (GM), moxifloxacin (MX), gatifloxacin (GT), and levofloxacin (LV) against S. pneumoniae 08-3, K. pneumoniae 09-23, and P. aeruginosa ATCC27853, 4 to 32 fold more potent than MX, GM, and LV against K. pneumoniae 09-21, and more active than or comparable to the four reference drugs against P. aeruginosa 09-32.
设计、合成并通过（1）H-NMR、MS 和 HRMS 对一系列新型 7-(3-氨基吡咯并[3,4-c]吡唑-5(2H,4H,6H)-基)-6-氟-4-氧代-1,4-二氢喹啉-3-羧酸衍生物进行了表征。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。一般来说，所有目标化合物对测试的革兰氏阴性菌株的活性都相当弱，但大多数化合物对金黄色葡萄球菌（包括耐甲氧西林金黄色葡萄球菌（MRSA）和表皮葡萄球菌（包括耐甲氧西林表皮葡萄球菌（MRSE））的生长具有良好的抑制作用（MIC：0.125-8μg/mL）。特别是化合物 9g 对肺炎链球菌 08-3、肺炎克雷伯菌 09-23 和铜绿假单胞菌 ATCC27853 的活性比吉米沙星（GM）、莫西沙星（MX）、加替沙星（GT）和左氧氟沙星（LV）强 2 至 32 倍，对肺炎克雷伯菌 09-21 的活性比 MX、GM 和 LV 强 4 至 32 倍，对铜绿假单胞菌 09-32 的活性与四种参考药物相当或优于四种参考药物。
