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We report here the inhibitory capacities of benzenesulphonamides, cyclitols and phenolic compounds 1-11 against three human CA isozymes (hCA I, hCA II and hCA VI) and bovine skeletal muscle carbonic anhydrase III (bCA III). The four isozymes showed quite diverse inhibition profiles with K-i values ranging from low micromolar to millimolar concentrations against all isoenzymes. Compound 5 and 6 had more powerful inhibitory action against hCA I and very similar action against hCA II and hCA VI as compared with acetazolamide (AZA) and sulphapyridine (SPD), specific CAIs. Probably the inhibition mechanism of the tested compounds is distinct of the sulphonamides with RSO2NH2 groups and similar to that of the coumarins/lacosamide, i.e. binding to a distinct part of the active site than that where sulphonamides bind. These data may lead to drug design campaigns of effective CAIs possessing a diverse inhibition mechanism compared to other sulphonamide/sulphamate inhibitors.", "publication_date": "2012-01-01", "resource_type": { "id": "publication-article", "title": { "en": "Journal article", "tr": "Dergi makalesi" } }, "rights": [ { "description": { "en": "The Creative Commons Attribution license allows re-distribution and re-use of a licensed work on the condition that the creator is appropriately credited." }, "icon": "cc-by-icon", "id": "cc-by-4.0", "props": { "scheme": "spdx", "url": "https://creativecommons.org/licenses/by/4.0/legalcode" }, "title": { "en": "Creative Commons Attribution 4.0 International" } } ], "title": "Carbonic anhydrase inhibitors: inhibition of human and bovine isoenzymes by benzenesulphonamides, cyclitols and phenolic compounds" }, "parent": { "access": { "owned_by": { "user": "1" } }, "communities": { "default": "be1a9c54-8a57-4004-beac-45f642d1fb86", "entries": [ { "access": { "member_policy": "open", "members_visibility": "public", "record_submission_policy": "open", "review_policy": "open", "visibility": "public" }, "children": { "allow": false }, "created": "2021-03-15T05:37:50.780180+00:00", "deletion_status": { "is_deleted": false, "status": "P" }, "id": "be1a9c54-8a57-4004-beac-45f642d1fb86", "links": {}, "metadata": { "curation_policy": "", "description": "", "page": "", "title": "TUBITAK Destekli Projelerden \u00c7\u0131kan Yay\u0131nlar Toplulu\u011fu " }, "revision_id": 0, "slug": "tubitak-destekli-proje-yayinlari", "updated": "2021-11-26T15:43:54.504251+00:00" } ], "ids": [ "be1a9c54-8a57-4004-beac-45f642d1fb86" ] }, "id": "84766", "pids": {} }, "pids": { "doi": { "identifier": "10.3109/14756366.2011.621122", "provider": "external" }, "oai": { "identifier": "oai:zenodo.org:84767", "provider": "oai" } }, "revision_id": 1, "stats": { "all_versions": { "data_volume": 3864.0, "downloads": 14, "unique_downloads": 14, "unique_views": 100, "views": 100 }, "this_version": { "data_volume": 3864.0, "downloads": 14, "unique_downloads": 14, "unique_views": 100, "views": 100 } }, "status": "published", "swh": {}, "updated": "2021-03-16T06:32:52.309277+00:00", "versions": { "index": 1, "is_latest": true } }