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1620458-09-4
  • names:

    (2R,4S,4aS)-11-fluoro-2,4-dimethyl-8-((S)-4-methyl-2-oxooxazolidin-3-yl)-1,2,4,4a-tetrahydro-2'H,6H-spiro[isoxazolo[4,5-g][1,4]oxazino[4,3-a]quinoline-5,5'-pyrimidine]-2',4',6'(1'H,3'H)-trione

  • CAS号:

    1620458-09-4

    MDL Number:
  • MF(分子式): C22H22FN5O7 MW(分子量): 487.44
  • EINECS: Reaxys Number:
  • Pubchem ID: Brand:BIOFOUNT
Zoliflodacin
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中文别名 (2R,4S,4aS)-11-fluoro-2,4-dimethyl-8-((S)-4-methyl-2-oxooxazolidin-3-yl)-1,2,4,4a-tetrahydro-2'H,6H-spiro[isoxazolo[4,5-g][1,4]oxazino[4,3-a]quinoline-5,5'-pyrimidine]-2',4',6'(1'H,3'H)-trione
英文别名 ETX0914; ETX-0914; ETX 0914; AZD0914; AZD-0914; AZD 0914; Zoliflodacin; CAS#1620458-09-4.
CAS号 1620458-09-4
SMILES O=C(NC(C12[C@]([C@H](C)O[C@H](C)C3)([H])N3C4=C(F)C(ON=C5N6C(OC[C@@H]6C)=O)=C5C=C4C2)=O)NC1=O
Inchi InChI=1S/C22H22FN5O7/c1-8-7-33-21(32)28(8)17-12-4-11-5-22(18(29)24-20(31)25-19(22)30)16-10(3)34-9(2)6-27(16)14(11)13(23)15(12)35-26-17/h4,8-10,16H,5-7H2,1-3H3,(H2,24,25,29,30,31)/t8-,9+,10-,16+/m0/s1
InchiKey ZSWMIFNWDQEXDT-ZESJGQACSA-N
分子式 Formula C22H22FN5O7
分子量 Molecular Weight 487.44
闪点 FP
熔点 Melting point
沸点 Boiling point
Polarizability极化度
密度 Density
蒸汽压 Vapor Pressure
溶解度Solubility
性状 Solid powder
储藏条件 Storage conditions Dry, dark and store at 0-4℃ for short term (days to weeks) or -20℃ for long term (Store correctly 2-3years).
产品说明 Zoliflodacin(CAS:1620458-09-4):仅限应用于工业或者科学研究过程中非医疗目的,不应用于人类或动物的临床诊断以及治过程疗,该产品非药用,非食用。
IntroductionZoliflodacin, also known as AZD0914 and ETX0914, is a new spiropyrimidinetrione bacterial DNA gyrase/topoisomerase inhibitor with potent in vitro antibacterial activity against key Gram-positive (Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus pyogenes, and Streptococcus agalactiae), fastidious Gram-negative (Haemophilus influenzae and Neisseria gonorrhoeae), atypical (Legionella pneumophila), and anaerobic (Clostridium difficile) bacterial species, including isolates with known resistance to fluoroquinolones. AZD0914 works via inhibition of DNA biosynthesis and accumulation of double-strand cleavages.
Application1
Application2
Application3
警示图
危险性 Warning
危险性警示
安全声明
安全防护
备注
[1]Foerster S, Golparian D, Jacobsson S, Hathaway LJ, Low N, Shafer WM, Althaus CL, Unemo M. Genetic Resistance Determinants, In Vitro Time-Kill Curve Analysis and Pharmacodynamic Functions for the Novel Topoisomerase II Inhibitor ETX0914 (AZD0914) in Neisseria gonorrhoeae. Front Microbiol. 2015 Dec 10;
6:1377. doi: 10.3389/fmicb.2015.01377. eCollection 2015. PubMed PMID: 26696986; PubMed Central PMCID: PMC4674575.
[3]Su XH, Wang BX, Le WJ, Liu YR, Wan C, Li S, Alm RA, Mueller JP, Rice PA. Multidrug resistant Neisseria gonorrhoeae from Nanjing are sensitive to killing by a novel DNA gyrase inhibitor, ETX0914 (AZD0914). Antimicrob Agents Chemother. 2015 Oct 19. pii: AAC.01211-15. [Epub ahead of print] PubMed PMID: 26482313.
[4]Biedenbach DJ, Huband MD, Hackel M, de Jonge BL, Sahm DF, Bradford PA. In Vitro Activity of AZD0914, a Novel Bacterial DNA Gyrase/Topoisomerase IV Inhibitor, against Clinically Relevant Gram-Positive and Fastidious Gram-Negative Pathogens. Antimicrob Agents Chemother. 2015 Oct;59(10):6053-63. doi: 10.1128/AAC.01016-15. Epub 2015 Jul 20. PubMed PMID: 26195518; PubMed Central PMCID: PMC4576048.
[5] Kern G, Palmer T, Ehmann DE, Shapiro AB, Andrews B, Basarab GS, Doig P, Fan J, Gao N, Mills SD, Mueller J, Sriram S, Thresher J, Walkup GK. Inhibition of Neisseria gonorrhoeae Type II Topoisomerases by the Novel Spiropyrimidinetrione AZD0914. J Biol Chem. 2015 Aug 21;290(34):20984-94. doi: 10.1074/jbc.M115.663534. Epub 2015 Jul 6. PubMed PMID: 26149691; PubMed Central PMCID: PMC4543657.
5: Unemo M, Ringlander J, Wiggins C, Fredlund H, Jacobsson S, Cole M. High in vitro susceptibility to the novel spiropyrimidinetrione ETX0914 (AZD0914) among 873 contemporary clinical Neisseria gonorrhoeae isolates from 21 European countries from 2012 to 2014. Antimicrob Agents Chemother. 2015 Sep;59(9):5220-5. doi: 10.1128/AAC.00786-15. Epub 2015 Jun 15. PubMed PMID: 26077246; PubMed Central PMCID: PMC4538562.
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