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The abnormal levels and activities are frequently\nassociated with various diseases therefore CAs have become an attractive target for the design\nof inhibitors or activators that can be used in the treatment of those diseases.<\/jats:p>\n<\/jats:sec>\n<jats:sec>\n<jats:title>Methods:<\/jats:title>\n<jats:p>Herein, we have designed and synthesized new benzimidazole-hydrazone derivatives to\ninvestigate the effects of these synthesized compounds on CA isoenzymes. Chemical structures of\nsynthesized compounds were confirmed by 1H NMR, 13C NMR, and HRMS. The synthetic derivatives\nwere screened for their inhibitory potential against carbonic anhydrase I and II by in vitro assay.<\/jats:p>\n<\/jats:sec>\n<jats:sec>\n<jats:title>Results:<\/jats:title>\n<jats:p>These compounds have IC50 values of 5.156-1.684 \u03bcM (hCA I) and 4.334-2.188 \u03bcM (hCA\nII). Inhibition types and Ki values of the compounds were determined. The Ki values of the compounds\nwere 5.44 \u00b1 0.14 \u03bcM-0.299 \u00b1 0.01 \u03bcM (hCA I) and 3.699 \u00b1 0.041 \u03bcM-1.507 \u00b1 0.01 \u03bcM\n(hCA II). The synthetic compounds displayed inhibitory action comparable to that of the clinically\nutilized reference substance, acetazolamide. According to this, compound 3p was the most effective\nmolecule with an IC50 value of 1.684 \u03bcM. Accordingly, the type of inhibition was noncompetitive\nand the Ki value was 0.299 \u00b1 0.01 \u03bcM.<\/jats:p>\n<\/jats:sec>\n<jats:sec>\n<jats:title>Conclusion:<\/jats:title>\n<jats:p>According to the in vitro test results, detailed protein-ligand interactions of the compound\n3p, which is more active against hCA I than standard azithromycin (AZM), were analyzed. In\naddition, the cytotoxic effects of the compounds on the L929 healthy cell line were evaluated.<\/jats:p>\n<\/jats:sec>","DOI":"10.2174\/1573406419666221222143530","type":"journal-article","created":{"date-parts":[[2022,12,26]],"date-time":"2022-12-26T04:03:04Z","timestamp":1672027384000},"page":"485-494","update-policy":"https:\/\/doi.org\/10.2174\/bsp_crossmark_policy","source":"Crossref","is-referenced-by-count":4,"title":["Synthesis and Molecular Docking of New N-Acyl Hydrazones-\nBenzimidazole as hCA I and II Inhibitors"],"prefix":"10.2174","volume":"19","author":[{"ORCID":"https:\/\/orcid.org\/0000-0001-8977-9775","authenticated-orcid":true,"given":"Kaan","family":"K\u00fc\u00e7\u00fcko\u011flu","sequence":"first","affiliation":[{"name":"Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Sel\u00e7uk University, Konya, Turkey"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-1879-1034","authenticated-orcid":true,"given":"Ulviye Acar","family":"\u00c7evik","sequence":"additional","affiliation":[{"name":"Department of\nPharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, Eski\u015fehir, 26470, Turkey"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Hayrunnisa","family":"Nadaroglu","sequence":"additional","affiliation":[{"name":"Department of Food\nTechnology, Erzurum Vocational Training School, Ataturk University, Erzurum, 25240, Turkey"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-8146-1663","authenticated-orcid":true,"given":"Ismail","family":"Celik","sequence":"additional","affiliation":[{"name":"Department of\nPharmaceutical Chemistry, Faculty of Pharmacy, Erciyes University, Kayseri, 38039, Turkey"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-1280-0019","authenticated-orcid":true,"given":"Ay\u015fen","family":"I\u015f\u0131k","sequence":"additional","affiliation":[{"name":"Department of Biochemistry,\nFaculty of Science, Sel\u00e7uk University, Konya, Turkey"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Hayrani Eren","family":"Bostanc\u0131","sequence":"additional","affiliation":[{"name":"Department of Biochemistry, Faculty of Pharmacy, Sivas\nCumhuriyet University, Sivas, Turkey"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Yusuf","family":"\u00d6zkay","sequence":"additional","affiliation":[{"name":"Department of\nPharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, Eski\u015fehir, 26470, Turkey"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Zafer As\u0131m","family":"Kaplanc\u0131kl\u0131","sequence":"additional","affiliation":[{"name":"Department of\nPharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, Eski\u015fehir, 26470, Turkey"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"965","reference":[{"key":"ref=1","doi-asserted-by":"publisher","first-page":"101","DOI":"10.1186\/s13065-019-0625-4","volume":"13","author":"Tahlan S.","year":"2019","unstructured":"Tahlan S.; Kumar S.; Narasimhan B.; Pharmacological significance of heterocyclic 1H-benzimidazole scaffolds: A review. 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