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Compounds <jats:bold>5\u2009a<\/jats:bold>\u2013<jats:bold>r<\/jats:bold> were found to selectively inhibit hCA\u2005II in the nanomolar range, while being less effective against the other hCA isoforms. As noted from the literature, sulfocoumarin (1,2\u2010benzoxathiine 2,2\u2010dioxide) acts as a \u201cprodrug\u201d inhibitor and is hydrolyzed by the esterase activity of hCA to form 2\u2010hydroxyphenylvinylsulfonic acid, which thereafter binds to the enzyme in a manner similar to that of coumarins and sulfoxocoumarins. All these sulfocoumarins (compounds <jats:bold>7\u2009a<\/jats:bold>\u2013<jats:bold>q<\/jats:bold>) were found to be very weak or ineffective as inhibitors of the housekeeping off\u2010target hCA isoforms I and II, and effectively inhibited the transmembrane tumor\u2010associated isoforms IX and XII in the high nanomolar to micromolar ranges. Further structural modifications of these molecules could be useful for the development of effective hCA inhibitors used for the treatment of glaucoma, epilepsy, and cancer.<\/jats:p>","DOI":"10.1002\/cmdc.201800180","type":"journal-article","created":{"date-parts":[[2018,4,20]],"date-time":"2018-04-20T03:00:16Z","timestamp":1524193216000},"page":"1165-1171","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":16,"title":["Synthesis and Biological Evaluation of 4\u2010Sulfamoylphenyl\/Sulfocoumarin Carboxamides as Selective Inhibitors of Carbonic Anhydrase Isoforms hCA\u2005II, IX, and XII"],"prefix":"10.1002","volume":"13","author":[{"given":"Srinivas","family":"Angapelly","sequence":"first","affiliation":[{"name":"Department of Medicinal Chemistry National Institute of Pharmaceutical Education &amp; Research (NIPER)  Hyderabad 500037 India"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Andrea","family":"Angeli","sequence":"additional","affiliation":[{"name":"NEUROFARBA Dept., Sezione di Scienze Farmaceutiche Universit\u00e0 degli Studi di Firenze  Via Ugo Schiff 6 50019 Sesto Fiorentino Florence Italy"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Arbaj Jabbar","family":"Khan","sequence":"additional","affiliation":[{"name":"Department of Medicinal Chemistry National Institute of Pharmaceutical Education &amp; Research (NIPER)  Hyderabad 500037 India"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"P. 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