Repositioning of 8-hydroxyquinoline derivatives as a new promising candidate for combating multidrug resistant Neisseria gonorrhoeae.

• DOI: 10.17179/excli2018-1602
• Publication Date: 2018-01-01
• Authors: Ratana Lawung; Rungrot Cherdtrak...; Sunanta Nabu; Supaluk Prachayas...; Chartchalerm Isar...; Prachayasittikul
• Keywords: Neisseria gonorrhoeae; Spectinomycin; Clioquinol; Quinolone

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