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"order": [], "total_bytes": 0 }, "metadata": { "creators": [ { "affiliations": [ { "name": "Gazi Univ, Dept Pharmaceut Chem, Fac Pharm, TR-06330 Ankara, Turkey" } ], "person_or_org": { "family_name": "Banoglu", "given_name": "Erden", "name": "Banoglu, Erden", "type": "personal" } }, { "affiliations": [ { "name": "Gazi Univ, Dept Pharmaceut Chem, Fac Pharm, TR-06330 Ankara, Turkey" } ], "person_or_org": { "family_name": "Celikoglu", "given_name": "Ersan", "name": "Celikoglu, Ersan", "type": "personal" } }, { "affiliations": [ { "name": "Univ Jena, Inst Pharm, Chair Pharmaceut Med Chem, Philosophenweg 14, D-07743 Jena, Germany" } ], "person_or_org": { "family_name": "Voelker", "given_name": "Susanna", "name": "Voelker, Susanna", "type": "personal" } }, { "affiliations": [ { "name": "Gazi Univ, Dept Pharmaceut Chem, Fac Pharm, TR-06330 Ankara, Turkey" } ], "person_or_org": { "family_name": "Olgac", "given_name": "Abdurrahman", "name": "Olgac, Abdurrahman", "type": "personal" } }, { "affiliations": [ { "name": "Univ Jena, Inst Pharm, Chair Pharmaceut Med Chem, Philosophenweg 14, D-07743 Jena, Germany" } ], "person_or_org": { "family_name": "Gerstmeier", "given_name": "Jana", "name": "Gerstmeier, Jana", "type": "personal" } }, { "affiliations": [ { "name": "Univ Jena, Inst Pharm, Chair Pharmaceut Med Chem, Philosophenweg 14, D-07743 Jena, Germany" } ], "person_or_org": { "family_name": "Garscha", "given_name": "Ulrike", "name": "Garscha, Ulrike", "type": "personal" } }, { "affiliations": [ { "name": "Gazi Univ, Dept Pharmaceut Chem, Fac Pharm, TR-06330 Ankara, Turkey" } ], "person_or_org": { "family_name": "Caliskan", "given_name": "Burcu", "name": "Caliskan, Burcu", "type": "personal" } }, { "person_or_org": { "family_name": "Schubert", "given_name": "Ulrich S.", "name": "Schubert, Ulrich S.", "type": "personal" } }, { "affiliations": [ { "name": "Univ Perugia, Dipartimento Sci Farmaceut, Via Liceo 1, I-06123 Perugia, Italy" } ], "person_or_org": { "family_name": "Carotti", "given_name": "Andrea", "name": "Carotti, Andrea", "type": "personal" } }, { "affiliations": [ { "name": "Univ Perugia, Dipartimento Sci Farmaceut, Via Liceo 1, I-06123 Perugia, Italy" } ], "person_or_org": { "family_name": "Macchiarulo", "given_name": "Antonio", "name": "Macchiarulo, Antonio", "type": "personal" } }, { "person_or_org": { "family_name": "Werz", "given_name": "Oliver", "name": "Werz, Oliver", "type": "personal" } } ], "description": "In this article, we report novel leukotriene (LT) biosynthesis inhibitors that may target 5-lipoxygenase-activating protein (FLAP) based on the previously identified isoxazole derivative (8). The design and synthesis was directed towards a subset of 4,5-diaryl-isoxazole-3-carboxylic acid derivatives as LT biosynthesis inhibitors. Biological evaluation disclosed a new skeleton of potential anti-inflammatory agents, exemplified by 39 and 40, which potently inhibit cellular 5-LO product synthesis (IC50 = 0.24 mu M, each) seemingly by targeting FLAP with weak inhibition on 5-LO (IC50 > 8 mu M). Docking studies and molecular dynamic simulations with 5-LO and FLAP provide valuable insights into potential binding modes of the inhibitors. Together, these diaryl-isoxazol-3-carboxylic acids may possess potential as leads for development of effective anti-inflammatory drugs through inhibition of LT biosynthesis. (C) 2016 Elsevier Masson SAS. All rights reserved.", "publication_date": "2016-01-01", "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": "4,5-Diarylisoxazol-3-carboxylic acids: A new class of leukotriene biosynthesis inhibitors potentially targeting 5-lipoxygenase-activating protein (FLAP)" }, "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": "60882", "pids": {} }, "pids": { "doi": { "identifier": "10.1016/j.ejmech.2016.02.027", "provider": "external" }, "oai": { "identifier": "oai:zenodo.org:60883", "provider": "oai" } }, "revision_id": 1, "stats": { "all_versions": { "data_volume": 4784.0, "downloads": 13, "unique_downloads": 13, "unique_views": 77, "views": 78 }, "this_version": { "data_volume": 4784.0, "downloads": 13, "unique_downloads": 13, "unique_views": 77, "views": 78 } }, "status": "published", "swh": {}, "updated": "2021-03-16T01:05:48.886418+00:00", "versions": { "index": 1, "is_latest": true } }