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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,*
1 Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China 2 The No.5 Hospital of Harbin, Harbin 150040, China 3 Beijing Key Laboratory of Drug Resistance Tuberculosis Research, Department of Pharmacology, Beijing Tuberculosis and Thoracic Tumor Research Institute, Beijing Chest Hospital, Capital Medical University, Beijing 101149, China
* Authors to whom correspondence should be addressed.
Received: 20 February 2013 / Revised: 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 (CC BY 3.0).

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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.

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