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Synthesis and In‐vitro Antibacterial Activity of 7‐(3‐Aminopyrrolo[3,4‐ c ]pyrazol‐5(2 H ,4 H ,6 H )‐yl)‐6‐fluoro‐4‐oxo‐1,4‐dihydroquinoline‐3‐carboxylic Acid Derivatives
Author(s) -
Guo Xin,
Bai XiaoGuang,
Li YiLiang,
An ZhiJiao,
Xu LeXing,
Han Liyou,
Liu MingLiang,
Guo HuiYuan,
Wang YuCheng
Publication year - 2011
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.201000160
Subject(s) - gemifloxacin , gatifloxacin , levofloxacin , potency , antibacterial activity , staphylococcus epidermidis , staphylococcus aureus , chemistry , moxifloxacin , in vitro , antibacterial agent , microbiology and biotechnology , stereochemistry , antibiotics , bacteria , biology , biochemistry , genetics
A series of novel 7‐(3‐aminopyrrolo[3,4‐ c ]pyrazol‐5(2 H ,4 H ,6 H )‐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.