Details

Autor(en) / Beteiligte

• Almolhim, Hanan
• Elhassanny, Ahmed E. M.
• Abutaleb, Nader S.
• Abdelsattar, Abdallah S.
• Seleem, Mohamed N.
• Carlier, Paul R.

Titel

Substituted salicylic acid analogs offer improved potency against multidrug-resistant Neisseria gonorrhoeae and good selectivity against commensal vaginal bacteria

Ist Teil von

• Scientific reports, 2023-09, Vol.13 (1), p.14468-14468, Article 14468

Ort / Verlag

London: Nature Publishing Group UK

Erscheinungsjahr

2023

Quelle

EZB Electronic Journals Library

Beschreibungen/Notizen

• Drug-resistant Neisseria gonorrhoeae represents a major threat to public health; without new effective antibiotics, untreatable gonococcal infections loom as a real possibility. In a previous drug-repurposing study, we reported that salicylic acid had good potency against azithromycin-resistant N. gonorrhoeae . We now report that the anti-gonococcal activity in this scaffold is easily lost by inopportune substitution, but that select substituted naphthyl analogs ( 3b , 3o and 3p ) have superior activity to salicylic acid itself. Furthermore, these compounds retained potency against multiple ceftriaxone- and azithromycin-resistant strains, exhibited rapid bactericidal activity against N. gonorrhoeae , and showed high tolerability to mammalian cells (CC 50  > 128 µg/mL). Promisingly, these compounds also show very weak growth inhibition of commensal vaginal bacteria.