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Molecules 2017, 22(7), 1171; doi:10.3390/molecules22071171

Synthesis and In Vitro Antimycobacterial and Antibacterial Activity of 8-OMe Ciprofloxacin-Hydrozone/Azole Hybrids

Key Laboratory of Hubei Province for Coal Conversion and New Carbon Materials, Wuhan University of Science and Technology, Wuhan 430081, China
Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
Pony Testing International Group (Wuhan), Wuhan 430000, China
Authors to whom correspondence should be addressed.
Received: 9 June 2017 / Accepted: 9 July 2017 / Published: 13 July 2017
(This article belongs to the Section Medicinal Chemistry)
View Full-Text   |   Download PDF [3748 KB, uploaded 13 July 2017]   |  


A series of novel 8-OMe ciprofloxacin (CPFX)-hydrazone/azole hybrids were designed, synthesized, and evaluated for their in vitro biological activities. Our results reveal that all of the hydrozone-containing hybrids (except for 7) show potency against Mycobacterium tuberculosis (MTB) H37Rv (minimum inhibitory concentration (MIC): <0.5 μM), which is better than the parent drug CPFX, and comparable to moxifloxacin and isoniazid, some of the tested Gram-positive strains (MIC: 0.06–4 μg/mL), and most Gram-negative strains (MIC: ≤0.03–4 μg/mL). View Full-Text
Keywords: 8-OMe ciprofloxacin; hybrids; synthesis; antimycobacterial; antibacterial 8-OMe ciprofloxacin; hybrids; synthesis; antimycobacterial; antibacterial

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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. (CC BY 4.0).

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Xu, Z.; Zhang, S.; Feng, L.-S.; Li, X.-N.; Huang, G.-C.; Chai, Y.; Lv, Z.-S.; Guo, H.-Y.; Liu, M.-L. Synthesis and In Vitro Antimycobacterial and Antibacterial Activity of 8-OMe Ciprofloxacin-Hydrozone/Azole Hybrids. Molecules 2017, 22, 1171.

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