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Molecules 2013, 18(4), 3872-3893; doi:10.3390/molecules18043872
Article

Synthesis, in Vitro Antimycobacterial and Antibacterial Evaluation of IMB-070593 Derivatives Containing a Substituted Benzyloxime Moiety

1, 2, 1,* , 1, 1, 1, 3 and 3,*
Received: 20 February 2013; in revised form: 21 March 2013 / Accepted: 22 March 2013 / Published: 28 March 2013
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Abstract: A series of novel IMB-070593 derivatives containing a substituted benzyloxime moiety and displaying a remarkable improvement in lipophilicity were synthesized and evaluated for their in vitro antimycobacterial and antibacterial activity. Our results reveal that the target compounds 19am have considerable Gram-positive activity (MIC: <0.008–32 µg/mL), although they are generally less active than the reference drugs against the Gram-negative strains. In particular, compounds 19h, 19j, 19k and 19m show good activity (MICs: <0.008–4 µg/mL) against all of the tested Gram-positive strains, including ciprofloxacin (CPFX)- and/or levofloxacin (LVFX)-resistant MSSA, MRSA and MSSE. Moreover, compound 19l (MIC: 0.125 µg/mL) is found to be 2–4 fold more active than the parent IMB070593, CPFX and LVFX against M. tuberculosis H37Rv ATCC 27294.
Keywords: IMB-070593 derivatives; benzyloxime; synthesis; antimycobacterial activity; antibacterial activity IMB-070593 derivatives; benzyloxime; synthesis; antimycobacterial activity; antibacterial activity
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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MDPI and ACS Style

Wei, Z.; Wang, J.; Liu, M.; Li, S.; Sun, L.; Guo, H.; Wang, B.; Lu, Y. Synthesis, in Vitro Antimycobacterial and Antibacterial Evaluation of IMB-070593 Derivatives Containing a Substituted Benzyloxime Moiety. Molecules 2013, 18, 3872-3893.

AMA Style

Wei Z, Wang J, Liu M, Li S, Sun L, Guo H, Wang B, Lu Y. Synthesis, in Vitro Antimycobacterial and Antibacterial Evaluation of IMB-070593 Derivatives Containing a Substituted Benzyloxime Moiety. Molecules. 2013; 18(4):3872-3893.

Chicago/Turabian Style

Wei, Zengquan; Wang, Jian; Liu, Mingliang; Li, Sujie; Sun, Lanying; Guo, Huiyuan; Wang, Bin; Lu, Yu. 2013. "Synthesis, in Vitro Antimycobacterial and Antibacterial Evaluation of IMB-070593 Derivatives Containing a Substituted Benzyloxime Moiety." Molecules 18, no. 4: 3872-3893.


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