Anti-Helicobacter pylori activity of ethoxzolamide
| العنوان: | Anti-Helicobacter pylori activity of ethoxzolamide |
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| المؤلفون: | Jose F. Garcia-Bustos, Rebecca J. Gorrell, Alexandra Tikhomirova, Terry Kwok, Despina Kotsanas, Anna Roujeinikova, Joyanta K. Modak, Richard L. Ferrero, Tony M. Korman, Mohammad M. Rahman, Claudiu T. Supuran |
| المصدر: | Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 34, Iss 1, Pp 1660-1667 (2019) Journal of Enzyme Inhibition and Medicinal Chemistry |
| بيانات النشر: | Informa UK Limited, 2019. |
| سنة النشر: | 2019 |
| مصطلحات موضوعية: | Glaucoma, Microbial Sensitivity Tests, Pharmacology, 01 natural sciences, Structure-Activity Relationship, Drug Discovery, Medicine, Mutation frequency, ethoxzolamide, Methazolamide, Dose-Response Relationship, Drug, Helicobacter pylori, Molecular Structure, biology, Ethoxzolamide, 010405 organic chemistry, business.industry, lcsh:RM1-950, General Medicine, biology.organism_classification, medicine.disease, mic/mbc, mutation frequency, Anti-Bacterial Agents, 0104 chemical sciences, genome sequencing, 010404 medicinal & biomolecular chemistry, lcsh:Therapeutics. Pharmacology, business, Acetazolamide, Research Paper, medicine.drug |
| الوصف: | 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, including the one that encodes undecaprenyl pyrophosphate synthase, a known target of sulphonamides. The data indicate that EZA impacts multiple targets in killing H. pylori. Our findings suggest that developing the approved anti-glaucoma drug EZA into a more effective anti-H. pylori agent may offer a faster and cost-effective route towards new antimicrobials with a novel mechanism of action. |
| تدمد: | 1475-6374 1475-6366 |
| الوصول الحر: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c1bc4fcf670ab2a5d192fe53c2a768a7Test https://doi.org/10.1080/14756366.2019.1663416Test |
| حقوق: | OPEN |
| رقم الانضمام: | edsair.doi.dedup.....c1bc4fcf670ab2a5d192fe53c2a768a7 |
| قاعدة البيانات: | OpenAIRE |
| تدمد: | 14756374 14756366 |
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