SML2744
Sitafloxacin sesquihydrate
≥98% (HPLC)
别名:
7-[(7S)-7-Amino-5-azaspiro[2.4]hept-5-yl]-8-chloro-6-fluoro-1-[(1R,2S)-2-fluorocyclopropyl]-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid, hydrate (2:3), DU 6859 sesquihydrate, DU 6859a sesquihydrate, DU-6859 sesquihydrate, DU-6859a sesquihydrate, DU6859 sesquihydrate, DU6859a sesquihydrate
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所有图片(1)
About This Item
经验公式（希尔记法）:
C19H18ClF2N3O3·1.5H2O
CAS号:
分子量:
436.84
MDL號碼:
分類程式碼代碼:
12352200
NACRES:
NA.77
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品質等級
化驗
≥98% (HPLC)
形狀
powder
儲存條件
desiccated
顏色
white to beige
溶解度
DMSO: 2 mg/mL, clear
儲存溫度
−20°C
SMILES 字串
F[C@@H]1[C@@H](C1)N2c3c(cc(c(c3Cl)N4C[C@H](C5(C4)CC5)N)F)C(=O)C(=C2)C(=O)O.O
InChI
1S/C19H18ClF2N3O3.H2O/c20-14-15-8(17(26)9(18(27)28)5-25(15)12-4-10(12)21)3-11(22)16(14)24-6-13(23)19(7-24)1-2-19;/h3,5,10,12-13H,1-2,4,6-7,23H2,(H,27,28);1H2/t10-,12+,13+;/m0./s1
InChI 密鑰
ANCJYRJLOUSQBW-JJZGMWGRSA-N
生化／生理作用
Orally active, 4th generation fluoroquinolone broad-spectrum antibiotic with dual DNA gyrase and topoisomerase IV inhibitory activity.
Sitafloxacin (DU-6859 or DU-6859a) is an orally active, fourth generation fluoroquinolone that exhibits broad-spectrum antibiotic activity against many Gram-positive, Gram-negative and anaerobic clinical isolates, including strains resistant to other fluoroquinolones, via dual inhibitory activity against bacterial DNA gyrase and topoisomerase IV (IC50 = 1.16 and 1.88 μg/mL against S. pneumoniae gyrA/B and parC/E, respectively). Sitafloxacin is active against methicillin-resistant staphylococci, Streptococcus pneumoniae and other streptococci with reduced susceptibility to levofloxacin and other quinolones and enterococci. Sitafloxacin also exhibits activity against clinical isolates of Klebsiella pneumoniae, Enterobacter cloacae, Pseudomonas aeruginosa as well as some activity against quinolone-resistant strains and Acinetobacter baumannii. Sitafloxacin in vitro activity against anaerobes is comparable to imipenem and metronidazole.
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
Ryoichi Hamasuna et al.
Microbial drug resistance (Larchmont, N.Y.), 24(1), 30-34 (2017-06-06)
Emergence of antimicrobial resistance in Neisseria gonorrhoeae is a major public health concern globally, and new antimicrobials for treatment of gonorrhea are imperative. In this study, the in vitro activity of sitafloxacin, a fluoroquinolone mainly used for respiratory tract or
Xiaomeng Dong et al.
International journal of clinical and experimental medicine, 8(5), 8135-8140 (2015-07-30)
To detect the in vitro activities of sitafloxacin alone and in combination with rifampin, colistin, sulbactam, and tigecycline against extensively drug-resistant Acinetobacter baumannii (XDR-A. baumannii). 24 XDR-A. baumannii strains were isolated from patients' specimens. Broth microdilution assay was used to
Y Onodera et al.
The Journal of antimicrobial chemotherapy, 44(4), 533-536 (1999-12-10)
The in-vitro inhibitory activities of sitafloxacin (DU-6859a) and other quinolones against Streptococcus pneumoniae DNA gyrase and topoisomerase IV were measured. IC50s of levofloxacin, ciprofloxacin, sparfloxacin and tosufloxacin against DNA gyrase were almost three to 12 times higher than those against
J F Tomayko et al.
Diagnostic microbiology and infectious disease, 20(1), 45-47 (1994-09-01)
The activity of DU-6859a, a new fluoroquinolone antimicrobial agent, was compared with that of ciprofloxacin by agar dilution susceptibility testing against enteric pathogens and multiresistant Escherichia coli. The results indicate that DU-6859a inhibits most of these organisms at concentrations similar
Lina Yi et al.
Journal of medical microbiology, 66(6), 770-776 (2017-06-10)
Purpose. Sitafloxacin (SFX) is a new fluoroquinolone (FQ) that has shown a strong bactericidal effect against Mycobacterium tuberculosis (Mtb) in vitro. However, data on SFX efficacy against Mtb with gyrA/B mutations and its epidemiological cut-off (ECOFF) value remain limited. Therefore
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