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Secondly, a series of new tetrabromo chalcone derivatives containing 4,7\u2010methanoisoindol\u20101,3\u2010dione (<jats:bold>2a\u2013i<\/jats:bold>) were synthesized from the addition of Br<jats:sub>2<\/jats:sub> to related chalcone derivatives (<jats:bold>1a\u2013i<\/jats:bold>). The structures of the new molecules (<jats:bold>2a\u2013i<\/jats:bold>) were confirmed by means of <jats:sup>1<\/jats:sup>H NMR, <jats:sup>13<\/jats:sup>C NMR and elemental analysis. Finally, the inhibitory effects of <jats:bold>2a\u2013i<\/jats:bold> on CA activities were investigated using the esterase method under <jats:italic>in vitro<\/jats:italic> conditions. The compounds <jats:bold>2a\u2013i<\/jats:bold> exhibited excellent inhibitory effects, in the low nanomolar range, with <jats:italic>K<\/jats:italic><jats:sub>i<\/jats:sub> values in the range of 11.30\u201321.22\u2009nM against hCA I and in the range of 8.21\u201312.86\u2009nM against hCA II. Our findings suggest that the new compounds <jats:bold>2a\u2013i<\/jats:bold> have superior inhibitory effect over acetazolamide (AZA), which is used as clinical CA inhibitor, with obtained <jats:italic>K<\/jats:italic><jats:sub>i<\/jats:sub> values of 34.50 and 28.93\u2009nM against the hCA I and II isozymes, respectively. In addition to the inhibition assays, molecular modeling approaches were implemented for prediction of the binding affinities of compounds <jats:bold>2a<\/jats:bold> and <jats:bold>2c<\/jats:bold>, which had the highest inhibition effects, against the hCA I and II isozymes.<\/jats:p><\/jats:sec>","DOI":"10.1002\/ardp.201700198","type":"journal-article","created":{"date-parts":[[2017,11,14]],"date-time":"2017-11-14T09:32:41Z","timestamp":1510651961000},"source":"Crossref","is-referenced-by-count":44,"title":["Synthesis and Carbonic Anhydrase Inhibition of Tetrabromo Chalcone Derivatives"],"prefix":"10.1002","volume":"350","author":[{"ORCID":"https:\/\/orcid.org\/0000-0001-8710-2912","authenticated-orcid":false,"given":"Umit M.","family":"Kocyigit","sequence":"first","affiliation":[{"name":"Vocational School of Health Services Cumhuriyet University Sivas Turkey"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Yakup","family":"Budak","sequence":"additional","affiliation":[{"name":"Department of Chemistry Faculty of Arts and Sciences Gaziosmanpasa University Tokat Turkey"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Fikret","family":"Elig\u00fczel","sequence":"additional","affiliation":[{"name":"Vocational School of Health Services Cumhuriyet University Sivas Turkey"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Parham","family":"Taslimi","sequence":"additional","affiliation":[{"name":"Department of Chemistry Faculty of Science Atat\u00fcrk University Erzurum Turkey"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Deryanur","family":"K\u0131l\u0131\u00e7","sequence":"additional","affiliation":[{"name":"Department of Chemistry Art and Science Faculty Aksaray University Aksaray Turkey"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"\u0130lhami","family":"Gul\u00e7in","sequence":"additional","affiliation":[{"name":"Department of Chemistry Faculty of Science Atat\u00fcrk University Erzurum Turkey"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Mustafa","family":"Ceylan","sequence":"additional","affiliation":[{"name":"Department of Chemistry Faculty of Arts and Sciences Gaziosmanpasa University Tokat Turkey"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"311","published-online":{"date-parts":[[2017,11,14]]},"reference":[{"key":"e_1_2_6_2_1","doi-asserted-by":"publisher","DOI":"10.1002\/jbt.21897"},{"key":"e_1_2_6_3_1","doi-asserted-by":"publisher","DOI":"10.1002\/ardp.201400257"},{"key":"e_1_2_6_4_1","doi-asserted-by":"publisher","DOI":"10.3109\/14756366.2012.670807"},{"key":"e_1_2_6_5_1","doi-asserted-by":"publisher","DOI":"10.1080\/14756366.2016.1244533"},{"key":"e_1_2_6_6_1","doi-asserted-by":"publisher","DOI":"10.25135\/acg.oc.4.16.05.418"},{"key":"e_1_2_6_7_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.bmcl.2010.07.038"},{"key":"e_1_2_6_8_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.indcrop.2015.05.034"},{"key":"e_1_2_6_9_1","doi-asserted-by":"publisher","DOI":"10.3109\/14756366.2015.1014476"},{"key":"e_1_2_6_10_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.ijbiomac.2016.10.096"},{"key":"e_1_2_6_11_1","doi-asserted-by":"crossref","first-page":"118","DOI":"10.1016\/j.bioorg.2016.12.001","volume":"70","author":"Kocyigit U. 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