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filingDate 2012-03-28-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 2013-10-30-04:00^^<http://www.w3.org/2001/XMLSchema#date>
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publicationDate 2013-10-30-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber CN-102633774-B
titleOfInvention Methionine or oxidized methionine modified Clinafloxacin and application thereof
abstract The invention discloses methionine or oxidized methionine modified Clinafloxacin, which refers to compounds shown in a formula I, wherein X is SO or SO2; Y is tert-butoxycarbonyl (Boc) or H.HZ, and HZ is HCl or trifluoroacetic acid (TFA); or X is S and Y is H.HCl. The compounds have certain bacteriostasis activity to gram-positive bacteria, such as Staphylococcus aureus, and gram-negative bacteria such as Escherichia coli, saimonella, and pseudomonas aeruginosa. The bacteriostasis activity to Staphylococcus aureus, pseudomonas aeruginosa and saimonella of the compounds TM2-1 (X is S and Y is H.HCl) and TM2-3 (X is SO2 and Y is H.HCl) is approximate to that of Clinafloxacin, and is superior to that of the known compound TM1-1 (X is S and Y is H.TFA). In the compound TM2-3 structure, S is in a maximum oxidation state, so that the compound TM2-3 is high in chemical stability. The Clinafloxacin derivatives can be used for preparing antibacterial medicaments, can provide more efficient and safe candidate medicaments for clinical treatment of infectious diseases, and meets various demands of clinical treatment.
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