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The exploitation of the <jats:italic>H. pylori<\/jats:italic> carbonic anhydrases (HpCAs) as promising pharmacological targets has been validated by the antibacterial activity of previously reported CA inhibitors due to the role of these enzymes in the bacterium survival in the gastric mucosa. The development of new HpCA inhibitors seems to be on the way to filling the existing antibiotics gap. Due to the recent evidence on the ability of the coumarin scaffold to inhibit microbial \u03b1\u2010CAs, a large library of derivatives has been developed by means of a pH\u2010regulated cyclization reaction of coumarin\u2010bearing acyl thiosemicarbazide intermediates. The obtained 1,3,4\u2010thiadiazoles (<jats:bold>10\u201318a,b<\/jats:bold>) and 1,2,4\u2010triazole\u20103\u2010thiones (<jats:bold>19\u201326a,b<\/jats:bold>) were found to strongly and selectively inhibit Hp\u03b1CA and computational studies were fundamental to gaining an understanding of the interaction networks governing the enzyme\u2013inhibitor complex. Antibacterial evaluations on <jats:italic>H. pylori<\/jats:italic> ATCC 43504 highlighted some compounds that maintained potency on a resistant clinical isolate. Also, their combinations with metronidazole decreased both the minimal inhibitory concentration\u00a0and minimal bactericidal concentration values of the antibiotic, with no synergistic effect.<\/jats:p>","DOI":"10.1002\/ardp.202400548","type":"journal-article","created":{"date-parts":[[2024,8,30]],"date-time":"2024-08-30T02:16:29Z","timestamp":1724984189000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":11,"title":["Cyclization of acyl thiosemicarbazides led to new <i>Helicobacter pylori<\/i> \u03b1\u2010carbonic anhydrase inhibitors"],"prefix":"10.1002","volume":"357","author":[{"ORCID":"https:\/\/orcid.org\/0000-0001-6459-7692","authenticated-orcid":false,"given":"Arzu","family":"Gumus","sequence":"first","affiliation":[{"name":"Department of Chemistry, Faculty of Science and Art Balikesir University Balikesir Turkey"},{"name":"Department of Neurofarba, Section of Pharmaceutical and Nutraceutical Sciences University of 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