Tuberculosis: Finding a New Potential Antimycobacterium Derivative in a Aldehyde–Arylhydrazone–Oxoquinoline Series

Current Microbiology(2012)

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摘要
Tuberculosis (TB) is a contagious disease caused by Mycobacterium tuberculosis , which remains a serious public health problem. The emergence of resistant bacterial strains has continuously increased and new treatment options are currently in need. In this work, we identified a new potential aldehyde–arylhydrazone–oxoquinoline derivative ( 4e ) with interesting chemical structural features that may be important for designing new anti-TB agents. This 1-ethyl- N ′-[(1E)-(5-nitro-2-furyl)methylene]-4-oxo-1,4-dihydroquinoline-3-carbohydrazide ( 4e ) presented an in vitro active profile against M. tuberculosis H37Rv strain (minimum inhibitory concentration, MIC = 6.25 μg/mL) better than other acylhydrazones described in the literature (MIC = 12.5 μg/mL) and close to other antitubercular agents currently on the market. The theoretical analysis showed the importance of several structural features that together with the 5-nitro-2-furyl group generated this active compound ( 4e ). This new compound and the analysis of its molecular properties may be useful for designing new and more efficient antibacterial drugs.
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关键词
Biopharmaceutics Classification System,Biopharmaceutics Classification System Class,Antitubercular Activity,Carbohydrazides,H37Rv Strain
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