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Zhang T.-T.,Zhejiang Xianju Pharmaceutical | Wang Z.,Zhejiang Xianju Pharmaceutical | Xu J.-J.,Zhejiang Xianju Pharmaceutical | Liu M.-L.,Peking Union Medical College
Chinese Journal of New Drugs | Year: 2012

Objective: To synthesize N-methyl-N-(2-hydroxyethyl)-N'-(2, 3-dihydroxypropyl)-5-(N-methylacetamido)-2, 4, 6-triiodoisophthalamide (STL-02). Methods: STL-02 was synthesized from 3-amino-5-(2, 3-dihydroxypropylcarbamoyl)-2, 4, 6-triiodobenzoic acid via acylation, acyl chlorination, acylamination, esterolysis and methylation. Results: The structure of STL-02 was identified by 1H-NMR and MS. Its purity was more than 98%. Conclusion: STL-02 has been synthesized; it is worth further safety evaluation.

Lv K.,Chinese Academy of Sciences | Sun Y.,Chinese Academy of Sciences | Sun L.,Chinese Academy of Sciences | Wei Z.,Chinese Academy of Sciences | And 3 more authors.
ChemMedChem | Year: 2012

A series of novel (R)/(S)-7-(3-alkoxyimino-2-aminomethyl-1-azetidinyl)fluoroquinolone derivatives were synthesized and evaluated for their invitro antibacterial activity against representative strains. Our results reveal that 12 of the target compounds generally show better activity (MIC: <0.008-0.5μgmL -1) against the tested Gram-positive strains including MRSA and MRSE than levofloxacin (LVFX, MIC: 0.125-8μgmL -1). Their activity is similar to that of gemifloxacin (GMFX, MIC: <0.008-4μgmL -1). However, they are generally less active than the two reference drugs against Gram-negative strains. Moreover, against clinical strains of S.aureus including MRSA and S.epidermidis including MRSE, the MIC 50 values (0.06-16μgmL -1) and MIC 90 values (0.5-32μgmL -1) of compounds 16w, y, and z are 2-8- and 2-16-fold less than LVFX, respectively, and 16w (MIC 90 range: 0.5-4μgmL -1) was also found to be more active than GMFX (MIC 90 range: 1-8μgmL -1). © 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

Feng Y.,Zhejiang Xianju Pharmaceutical | Zhang C.,Zhejiang University
Acta Crystallographica Section E: Structure Reports Online | Year: 2010

In the title compound, C15H14O3S, the dihedral angle between the two benzene rings is 59.3 (8)°. The crystal structure is stabilized by weak intermolecular C - H⋯π interactions between the benzene rings and the central ethyl-ene bridge, and a weak non-classical C - H⋯O hydrogen bond occurs in the structure. © 2010.

Lv K.,Peking Union Medical College | Wu J.,Zhejiang Xianju Pharmaceutical | Wang J.,No. 5 Hospital of Harbin | Liu M.,Peking Union Medical College | And 4 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2013

We report herein the synthesis of a series of 7-[3-alkoxyimino-4-(methyl) aminopiperidin-1-yl]quinolone/naphthyridone derivatives. In vitro antibacterial activity of these derivatives was evaluated against representative strains, and compared with ciprofloxacin (CPFX), levofloxacin (LVFX) and gemifloxacin (GMFX). The results reveal that all of the target compounds 19a-c and 20 have considerable Gram-positive activity, although they are generally less active than the reference drugs against the Gram-negative strains with some exceptions. Especially, novel compounds 19a2, 19a4 and 19a5 were found to show strong antibacterial activity (MICs: <0.008-0.5 μg/mL) against all of the tested 15 Gram-positive strains including MRSA, LVFX- and GMFX-resistant MRSE, and CPFX-, LVFX- and GMFX-resistant MSSA. © 2013 Elsevier Ltd. All rights reserved.

Huang J.,Peking Union Medical College | Wang M.,Peking Union Medical College | Wang B.,Capital Medical University | Wu Z.,Peking Union Medical College | And 7 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2016

A series of novel 1-(6-amino-3,5-difluoropyridin-2-yl)fluoroquinolone derivatives containing an oxime functional moiety were synthesized and evaluated for their biological activity. Our results reveal that compounds 9a-9c have considerable activity against both of MTB H37Rv ATCC 27294 (MICs: 3.81-7.13 μg/mL) and methicillin-sensitive Staphylococcus aureus strains (MICs: <0.008-0.5 μg/mL). © 2016 Elsevier Ltd. All rights reserved.

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