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In this study, we present novel 2\u2010phenylbenzothiazole derivatives featuring heteroaryl sulfonamide end\u2010capping substructures as inhibitors of human mPGES\u20101, with IC<jats:sub>50<\/jats:sub> values in the range of 0.72\u20133.40\u2009\u00b5M in a cell\u2010free assay of PGE<jats:sub>2<\/jats:sub> formation. Notably, compound <jats:bold>21<\/jats:bold>, featuring a quinoxalinedione ring in its sulfonamide segment, effectively suppresses PGE<jats:sub>2<\/jats:sub> biosynthesis at a low micromolar concentration (IC<jats:sub>50<\/jats:sub>\u2009=\u20090.72\u2009\u00b5M) with exceptional selectivity against cyclooxygenase (COX)\u20101, COX\u20102, 5\u2010lipoxygenase (5\u2010LOX), and FLAP. This compound offers a novel chemical scaffold for developing safer and more effective anti\u2010inflammatory agents.<\/jats:p>","DOI":"10.1002\/ardp.202400756","type":"journal-article","created":{"date-parts":[[2025,1,16]],"date-time":"2025-01-16T12:33:42Z","timestamp":1737030822000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":1,"title":["2\u2010Phenylbenzothiazoles featuring heteroaryl sulfonamide end\u2010capping substructures as developable mPGES\u20101 inhibitors"],"prefix":"10.1002","volume":"358","author":[{"given":"Tansu","family":"Yal\u00e7\u0131n","sequence":"first","affiliation":[{"name":"Department of Pharmaceutical Chemistry, Faculty of Pharmacy Gazi University Ankara Turkey"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-8364-4236","authenticated-orcid":false,"given":"Paul M.","family":"Jordan","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutical\/Medicinal Chemistry, Institute of Pharmacy Friedrich Schiller University Jena Jena Germany"},{"name":"Jena Center for Soft Matter (JCSM) Friedrich Schiller University Jena Jena Germany"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-8470-4942","authenticated-orcid":false,"given":"Abdurrahman","family":"Ol\u011fa\u00e7","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutical Chemistry, Faculty of Pharmacy Gazi University Ankara Turkey"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Philipp","family":"Dahlke","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutical\/Medicinal Chemistry, Institute of Pharmacy Friedrich Schiller University Jena Jena Germany"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-8916-2492","authenticated-orcid":false,"given":"Tu\u011f\u00e7e G\u00fcr","family":"Maz","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutical Chemistry, Faculty of Pharmacy Gazi University Ankara Turkey"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-4737-1733","authenticated-orcid":false,"given":"Erden","family":"Banoglu","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutical Chemistry, Faculty of Pharmacy Gazi University Ankara Turkey"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-5064-4379","authenticated-orcid":false,"given":"Oliver","family":"Werz","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutical\/Medicinal Chemistry, Institute of Pharmacy Friedrich Schiller University Jena Jena Germany"},{"name":"Jena Center for Soft Matter (JCSM) Friedrich Schiller University Jena Jena Germany"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-2391-5644","authenticated-orcid":false,"given":"Burcu","family":"\u00c7al\u0131\u015fkan","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutical Chemistry, Faculty of Pharmacy Gazi University Ankara Turkey"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"311","published-online":{"date-parts":[[2025,1,16]]},"reference":[{"key":"e_1_2_8_2_1","doi-asserted-by":"publisher","DOI":"10.1007\/s000110050284"},{"key":"e_1_2_8_3_1","doi-asserted-by":"publisher","DOI":"10.1080\/17512433.2018.1516143"},{"key":"e_1_2_8_3_2","doi-asserted-by":"publisher","DOI":"10.2131\/jts.44.373"},{"key":"e_1_2_8_3_3","doi-asserted-by":"publisher","DOI":"10.1038\/s41569-020-0366-z"},{"key":"e_1_2_8_4_1","first-page":"2","volume":"51","author":"Bolten W. 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