{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2025,11,30]],"date-time":"2025-11-30T09:14:52Z","timestamp":1764494092305,"version":"build-2065373602"},"reference-count":48,"publisher":"MDPI AG","issue":"9","license":[{"start":{"date-parts":[[2020,4,29]],"date-time":"2020-04-29T00:00:00Z","timestamp":1588118400000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"DOI":"10.13039\/501100004006","name":"Bilimsel Ara\u015ftirma Projeleri Birimi, Istanbul \u00dcniversitesi","doi-asserted-by":"publisher","award":["TSA-2019-30535"],"award-info":[{"award-number":["TSA-2019-30535"]}],"id":[{"id":"10.13039\/501100004006","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["IJMS"],"abstract":"<jats:p>Due to the increasing resistance of currently used antimicrobial drugs, there is an urgent problem for the treatment of cholera disease, selective inhibition of the \u03b1-class carbonic anhydrases (CA, EC 4.2.1.1) from the pathogenic bacterium Vibrio cholerae (VcCA) presents an alternative therapeutic target. In this study, a series of hydrazone derivatives, carrying the 2-(hydrazinocarbonyl)-3-phenyl-1H-indole-5-sulfonamide scaffold, have been evaluated as inhibitors of the VcCA with molecular modeling studies. The results suggest that these compounds may bind to the active site of VcCA. To verify this, VcCA enzyme inhibition studies were performed and as predicted most of the tested compounds displayed potent inhibitory activities against VcCA with three compounds showing KI values lower than 30 nM. In addition, all these compounds showed selectivity for VcCA and the off-targets hCA I and II.<\/jats:p>","DOI":"10.3390\/ijms21093131","type":"journal-article","created":{"date-parts":[[2020,4,29]],"date-time":"2020-04-29T13:23:45Z","timestamp":1588166625000},"page":"3131","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":7,"title":["Novel Indole-Based Hydrazones as Potent Inhibitors of the \u03b1-class Carbonic Anhydrase from Pathogenic Bacterium Vibrio cholerae"],"prefix":"10.3390","volume":"21","author":[{"ORCID":"https:\/\/orcid.org\/0000-0001-9928-4733","authenticated-orcid":false,"given":"K\u00fcbra","family":"Demir-Yaz\u0131c\u0131","sequence":"first","affiliation":[{"name":"Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Istanbul University, Beyazit, 34116 Istanbul, Turkey"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-3680-1945","authenticated-orcid":false,"given":"\u00d6zlen","family":"G\u00fczel-Akdemir","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Istanbul University, Beyazit, 34116 Istanbul, Turkey"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-1470-7192","authenticated-orcid":false,"given":"Andrea","family":"Angeli","sequence":"additional","affiliation":[{"name":"Neurofarba Department, Section of Pharmaceutical and Nutriceutical Sciences, Universit\u00e0 degli Studi di Firenze, Via U. Schiff 6, 50019 Sesto Fiorentino (Florence), Italy"},{"name":"Centre of Advanced Research in Bionanoconjugates and Biopolymers Department, \u201cPetru Poni\u201d Institute of Macromolecular Chemistry, 700487 Iasi, Romania"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-4262-0323","authenticated-orcid":false,"given":"Claudiu T.","family":"Supuran","sequence":"additional","affiliation":[{"name":"Neurofarba Department, Section of Pharmaceutical and Nutriceutical Sciences, Universit\u00e0 degli Studi di Firenze, Via U. Schiff 6, 50019 Sesto Fiorentino (Florence), Italy"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-8416-0471","authenticated-orcid":false,"given":"Atilla","family":"Akdemir","sequence":"additional","affiliation":[{"name":"Computer-aided Drug Discovery Laboratory, Department of Pharmacology, Faculty of Pharmacy, Bezmialem Vakif University, Fatih, 34093 Istanbul, Turkey"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"1968","published-online":{"date-parts":[[2020,4,29]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"2466","DOI":"10.1016\/S0140-6736(12)60436-X","article-title":"Cholera","volume":"Volume 379","author":"Harris","year":"2012","journal-title":"Proceedings of the The Lancet"},{"key":"ref_2","doi-asserted-by":"crossref","first-page":"1","DOI":"10.1038\/s41598-019-41883-x","article-title":"High quality reference genomes for toxigenic and non-toxigenic Vibrio cholerae serogroup O139","volume":"9","author":"Dorman","year":"2019","journal-title":"Sci. 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