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These thiadiazol derivatives were evaluated against four physiologically relevant CA isoforms (hCA I, II, IX, and XII), and demonstrated intriguing inhibitory activity against CA II with K<jats:sub>i<\/jats:sub> values in the range of 2.4\u201331.6\u2005nM. Besides hCA II, also hCA XII activity was potently inhibited by some of the derivatives (K<jats:sub>i<\/jats:sub>=1.5\u201388.5\u2005nM), producing dual inhibitors of both isoforms. Notably, compound <jats:bold>17<\/jats:bold> was the most potent dual CA II (K<jats:sub>i<\/jats:sub>=3.1\u2005nM) and XII (K<jats:sub>i<\/jats:sub>=1.5\u2005nM) inhibitor with a significant selectivity ratio over CA I and IX isoforms. In conclusion, although all compounds exhibited preferential activity towards hCA II, the nature of the substituents at the tail part of the main scaffold influenced the activity and selectivity toward other isoforms.<\/jats:p>","DOI":"10.1002\/cmdc.202200056","type":"journal-article","created":{"date-parts":[[2022,3,10]],"date-time":"2022-03-10T00:29:33Z","timestamp":1646872173000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":7,"title":["A Series of Thiadiazolyl\u2010Benzenesulfonamides Incorporating an Aromatic Tail as Isoform\u2010Selective, Potent Carbonic Anhydrase II\/XII Inhibitors"],"prefix":"10.1002","volume":"17","author":[{"ORCID":"https:\/\/orcid.org\/0000-0003-4737-1733","authenticated-orcid":false,"given":"Erden","family":"Banoglu","sequence":"first","affiliation":[{"name":"Department of Pharmaceutical Chemistry Faculty of Pharmacy Gazi University  Ta\u00e7 Sok. 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No:3 Yenimahalle 06560 Ankara Turkey"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Daniela","family":"Vullo","sequence":"additional","affiliation":[{"name":"Department of NEUROFARBA Section of Pharmaceutical and Nutraceutical Sciences University of Florence  Polo Scientifico, Via Ugo Schiff 6 50019 Sesto Fiorentino Firenze Italy"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Alessandro","family":"Bonardi","sequence":"additional","affiliation":[{"name":"Department of NEUROFARBA Section of Pharmaceutical and Nutraceutical Sciences University of Florence  Polo Scientifico, Via Ugo Schiff 6 50019 Sesto Fiorentino Firenze Italy"},{"name":"Department of NEUROFARBA Section of Pharmaceutical and Nutraceutical Sciences Laboratory of Molecular Modeling Cheminformatics &amp; QSAR University of Florence  Polo Scientifico, Via U. 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