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.pdfVIP
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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
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
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