Repositioning of 8-hydroxyquinoline derivatives as a new promising candidate for combating multidrug resistant Neisseria gonorrhoeae
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Date
2018-08-23
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Abstract
The multidrug resistance of Neisseria gonorrhoeae becomes a public health problem worldwide,
especially the strain H041 that showed the decrease susceptibility to ceftriaxone which is the last
resort for gonorrhea treat- ment. Therefore, the simultaneous discovery and development of a new
compound to fight this pathogen is ur- gently required. In this study, 8-hydroxyquinoline (8HQ) and
derivatives were evaluated for their antimicrobial activities against the gonococcal pathogen using
spectinomycin as the reference drug. The results showed that 8HQ derivatives gave an excellent
antimicrobial potency. Particularly, the dihalogenated 8HQ (iodoquinol, clio- quinol and
5,7-diCl-8HQ) exerted the high activity with MIC range of 0.08-0.15 µM, 0.10-0.20 µM and 0.28-
0.56 µM, respectively, compared with the reference drug (MIC = 16 µg/mL or 48.14 µM). Moreover,
these compounds were also shown to be non-cytotoxic/very high safety index. The findings reveal
that these three
compounds could be further developed as a new antimicrobial agent for fighting the gonorrheal
disease.
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Keywords
Neisseria gonorrhoeae, Antimicrobial resistance, Antibacterial activity, 8-hydroxyquinoline and derivatives