{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,3,20]],"date-time":"2026-03-20T03:06:13Z","timestamp":1773975973205,"version":"3.50.1"},"reference-count":28,"publisher":"Wiley","issue":"8","license":[{"start":{"date-parts":[[2022,4,28]],"date-time":"2022-04-28T00:00:00Z","timestamp":1651104000000},"content-version":"vor","delay-in-days":0,"URL":"http:\/\/onlinelibrary.wiley.com\/termsAndConditions#vor"}],"content-domain":{"domain":["onlinelibrary.wiley.com"],"crossmark-restriction":true},"short-container-title":["Archiv der Pharmazie"],"published-print":{"date-parts":[[2022,8]]},"abstract":"<jats:title>Abstract<\/jats:title><jats:p>Saccharin is a cyclic secondary sulfonamide, which is a selective inhibitor of the tumor\u2010associated carbonic anhydrase (CA; EC 4.2.1.1) enzymes CA IX and CA XII compared to many primary sulfonamides. In this study, new saccharin\u20101,2,3\u2010triazole and saccharin\u20101,2,4\u2010oxadiazole hybrids were synthesized. All the newly synthesized molecules were screened for their CA\u2010inhibitory activity against four important human CA (hCA) isoforms: hCA I, hCA II, hCA IX, and hCA XII. Compounds <jats:bold>8a<\/jats:bold> and <jats:bold>8f<\/jats:bold> emerged as potent hCA II inhibitors (<jats:italic>K<\/jats:italic><jats:sub>i<\/jats:sub>\u2009=\u20093\u2009\u00b5M). Compounds <jats:bold>6d<\/jats:bold>, <jats:bold>6e<\/jats:bold> and <jats:bold>7a, 7b<\/jats:bold> were highly selective against hCA IX (<jats:bold>6d, 6e<\/jats:bold>) and hCA II (<jats:bold>7a, 7b<\/jats:bold>), with moderate inhibitory activity. The activity of these compounds was further confirmed by performing in silico docking studies against hCA II and hCA IX.<\/jats:p>","DOI":"10.1002\/ardp.202200019","type":"journal-article","created":{"date-parts":[[2022,4,29]],"date-time":"2022-04-29T03:35:55Z","timestamp":1651203355000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":5,"title":["Design, synthesis, SAR, and biological evaluation of saccharin\u2010based hybrids as carbonic anhydrase inhibitors"],"prefix":"10.1002","volume":"355","author":[{"given":"Krishna K.","family":"Chinchilli","sequence":"first","affiliation":[{"name":"Department of Medicinal Chemistry National Institute of Pharmaceutical Education and Research (NIPER) Hyderabad India"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Venkata N.","family":"Royyala","sequence":"additional","affiliation":[{"name":"Department of Medicinal Chemistry National Institute of Pharmaceutical Education 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