Anti-Helicobacter pylori activity of ethoxzolamide.
Joyanta K Modak, Alexandra Tikhomirova, Rebecca J Gorrell, Mohammad M Rahman, Despina Kotsanas, Tony M Korman, Jose Garcia-Bustos, Terry Kwok, Richard L Ferrero, Claudiu T Supuran, Anna Roujeinikova
Journal of Enzyme Inhibition and Medicinal Chemistry | Taylor & Francis Open | Published : 2019
Ethoxzolamide (EZA), acetazolamide, and methazolamide are clinically used sulphonamide drugs designed to treat non-bacteria-related illnesses (e.g. glaucoma), but they also show antimicrobial activity against the gastric pathogen Helicobacter pylori. EZA showed the highest activity, and was effective against clinical isolates resistant to metronidazole, clarithromycin, and/or amoxicillin, suggesting that EZA kills H. pylori via mechanisms different from that of these antibiotics. The frequency of single-step spontaneous resistance acquisition by H. pylori was less than 5 × 10-9, showing that resistance to EZA does not develop easily. Resistance was associated with mutations in three genes, i..View full abstract