| 词条 | Nemonoxacin |
| 释义 |
| ImageFile = Nemonoxacin structure.svg | ImageSize = 220px | IUPACName = 7-[(3S,5S)-3-Amino-5-methyl-1-piperidinyl]-1-cyclopropyl-8-methoxy-4-oxo-1,4-dihydro-3-quinolinecarboxylic acid | OtherNames = |Section1={{Chembox Identifiers | CASNo = | PubChem = 11993740 | ChemSpiderID = 10166207 | SMILES = C[C@H]1C[C@H](N)CN(C1)c2ccc3c(c2OC)n(C4CC4)cc(c3=O)C(=O)O | InChI = 1/C20H25N3O4/c1-11-7-12(21)9-22(8-11)16-6-5-14-17(19(16)27-2)23(13-3-4-13)10-15(18(14)24)20(25)26/h5-6,10-13H,3-4,7-9,21H2,1-2H3,(H,25,26)/t11-,12-/m0/s1 | InChIKey = AVPQPGFLVZTJOR-RYUDHWBXBZ | StdInChI = 1S/C20H25N3O4/c1-11-7-12(21)9-22(8-11)16-6-5-14-17(19(16)27-2)23(13-3-4-13)10-15(18(14)24)20(25)26/h5-6,10-13H,3-4,7-9,21H2,1-2H3,(H,25,26)/t11-,12-/m0/s1 | StdInChIKey = AVPQPGFLVZTJOR-RYUDHWBXSA-N |Section2={{Chembox Properties | C=20 | H=25 | N=3 |O=4 | Appearance = | Density = | MeltingPt = | BoilingPt = | Solubility = |Section3={{Chembox Hazards | MainHazards = | FlashPt = | AutoignitionPt = |Section6={{Chembox Pharmacology | ATCCode_prefix = J01 | ATCCode_suffix = MB08 }}Nemonoxacin is a non-fluorinated quinolone antibiotic undergoing clinical trials.[1] It has the same mechanism of action as fluouroquinolones; it inhibits DNA gyrase, preventing DNA synthesis, gene duplication, and cell division. At the end of 2016, it had reached market in Taiwan, Russia, the Commonwealth Independent States, Turkey, mainland China,[2] and Latin America[3] under the brand name Taigexyn. Nemonoxacin has completed phase 2 trials in the USA and has moved on to phase 3 trials.[4] The U.S. Food and Drug Administration (FDA) has granted nemonoxacin qualified infectious disease product (QIDP) and fast track designations for community-acquired bacterial pneumonia (CAP) and acute bacterial skin and skin-structure infections (ABSSSI).[5] Nemonoxacin has a broad spectrum of activity against Gram-positive, Gram-negative, and atypical pathogens, including activity against methicillin-resistant Staphylococcus aureus (MRSA) (MIC90 1 g/ml) and vancomycin-resistant pathogens.[6][7] However, it was less active against Gram-negative pathogens such as Escherichia coli, Proteus mirabilis, and Pseudomonas aeruginosa, with MIC90 values of 32, 16, and 32 g/ml, respectively.[8] The new drug also is effective against C.difficile isolates that are resistant to other quinolones,[9] and is more potent than levofloxacin or moxifloxacin.[10] References1. ^{{cite journal|pmid=22650326|year=2012|author1=Guo|first1=B|title=Safety and clinical pharmacokinetics of nemonoxacin, a novel non-fluorinated quinolone, in healthy Chinese volunteers following single and multiple oral doses|journal=Clinical Drug Investigation|volume=32|issue=7|pages=475–86|last2=Wu|first2=X|last3=Zhang|first3=Y|last4=Shi|first4=Y|last5=Yu|first5=J|last6=Cao|first6=G|last7=Zhang|first7=J|doi=10.2165/11632780-000000000-00000}} {{QuinoloneAntiBiotics}}{{Antibiotic-stub}}2. ^{{cite web|url=http://www.news-medical.net/news/20151216/TaiGen-releases-Taigexyn-(nemonoxacin)-capsules-in-Taiwan.aspx|title=TaiGen releases Taigexyn (nemonoxacin) capsules in Taiwan|date=16 December 2015|publisher=}} 3. ^{{cite web|url=http://www.prnewswire.com/news-releases/taigen-biotechnology-out-licenses-taigexyn-nemonoxacin-to-productos-cientificos-for-the-latin-american-market-300318179.html|title=TaiGen Biotechnology Out-Licenses Taigexyn® (Nemonoxacin) to Productos Científicos for the Latin American Market|first=TaiGen|last=Biotechnology|publisher=}} 4. ^{{cite web|url=https://clinicaltrials.gov/ct2/show/NCT02205112|title=A Phase III Study to Evaluate the Efficacy and Safety of Intravenous Infusion of Nemonoxacin in Treating CAP - Full Text View - ClinicalTrials.gov|publisher=}} 5. ^{{cite web|url=http://www.news-medical.net/news/20131223/FDA-grants-QIDP-and-Fast-Track-designations-to-TaiGens-nemonoxacin.aspx|title=FDA grants QIDP and Fast Track designations to TaiGen's nemonoxacin|date=23 December 2013|publisher=}} 6. ^{{cite journal | author = Lauderdale TL, Shiau YR, Lai JF, Chen HC, King CH | year = 2010 | title = Comparative in vitro activities of nemonoxacin (TG-873870), a novel nonfluorinated quinolone, and other quinolones against clinical isolates | url = | journal = Antimicrob. Agents Chemother. | volume = 54 | issue = | pages = 1338–1342 | doi=10.1128/aac.01197-09| pmc = 2825994}} 7. ^{{cite journal | author = Adam HJ, Laing NM, King CR, Lulashnyk B, Hoban DJ, Zhanel GG | year = 2009 | title = In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates | url = | journal = Antimicrob. Agents Chemother. | volume = 53 | issue = | pages = 4915–4920 | doi=10.1128/aac.00078-09| pmc = 2772340}} 8. ^{{cite journal | author = van Rensburg DJ, Perng RP, Mitha IH, Bester AJ, Kasumba J, Wu RG, Ho ML, Chang LW, Chung DT, Chang YT, King CH, Hsu MC | year = 2010 | title = Efficacy and safety of nemonoxacin versus levofloxacin for community-acquired pneumonia | url = | journal = Antimicrob. Agents Chemother. | volume = 54 | issue = | pages = 4098–4106 | doi=10.1128/aac.00295-10| pmc = 2944601}} 9. ^{{cite journal |pmc=3393409|year=2012|author1=Liao|first1=C. H.|title=Characterizations of Clinical Isolates of Clostridium difficile by Toxin Genotypes and by Susceptibility to 12 Antimicrobial Agents, Including Fidaxomicin (OPT-80) and Rifaximin: A Multicenter Study in Taiwan|journal=Antimicrobial Agents and Chemotherapy|volume=56|issue=7|pages=3943–3949|last2=Ko|first2=W. C.|last3=Lu|first3=J. J.|last4=Hsueh|first4=P. R.|doi=10.1128/AAC.00191-12|pmid=22508299}} 10. ^{{cite journal |pmc=3697386|year=2013|author1=Liang|first1=W|title=Pharmacokinetics and Pharmacodynamics of Nemonoxacin against Streptococcus pneumoniae in an in Vitro Infection Model|journal=Antimicrobial Agents and Chemotherapy|volume=57|issue=7|pages=2942–2947|last2=Chen|first2=Y. C.|last3=Cao|first3=Y. R.|last4=Liu|first4=X. F.|last5=Huang|first5=J|last6=Hu|first6=J. L.|last7=Zhao|first7=M|last8=Guo|first8=Q. L.|last9=Zhang|first9=S. J.|last10=Wu|first10=X. J.|last11=Zhu|first11=D. M.|last12=Zhang|first12=Y. Y.|last13=Zhang|first13=J|doi=10.1128/AAC.01098-12|pmid=23587953}} 5 : Cyclopropanes|Piperidines|Quinolone antibiotics|Carboxylic acids|Phenol ethers |
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