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 derivatives7 -合成和体外抗菌活性(3-amino-6,7-dihydro-2-methyl-2h-pyrazolo[4、3 c]pyridin-5(4 h)- yl)氟喹诺酮类衍生品.pdf

Molecules 2011, 16, 2626-2635; doi:10.3390/molecule OPEN ACCESS molecules ISSN 1420-3049 /journal/molecules Article 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 Xin Guo 1,2, Ming Liang Liu 1, Hui Yuan Guo 1, Yu Cheng Wang 1 and Ju Xian Wang 1,* 1 Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China 2 College of Pharmaceutical Sciences, Southwest University, Chongqing 400715, China; E-Mail:guoxincq@ * Author to whom correspondence should be addressed; E-Mail: wyc9999@; Tel.: +86-10 Fax: +86-10 Received: 31 December 2010; in revised form: 16 March 2011 / Accepted: 18 March 2011 / Published: 22 March 2011 Abstract: 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), c