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The results showed that compounds <jats:bold>3f<\/jats:bold>, <jats:bold>3h<\/jats:bold>, <jats:bold>3l<\/jats:bold>, and <jats:bold>3p<\/jats:bold> have an excellent COX\u20102 selectivity index. Moreover, they showed potent 5\u2010LOX inhibitory activity relative to celecoxib and zileuton, as positive controls. These promising candidates were further investigated for anti\u2010inflammatory activity using the carrageenan\u2010induced rat paw edema method and ulcerogenic liability. The results showed no ulceration, which implies their gastric safety profile. Moreover, these compounds were evaluated for prostaglandin (PGE2) production in rat serum. Molecular docking in the COX\u20102 and 5\u2010LOX active sites was performed to rationalize their anti\u2010inflammatory activities. Strong binding interactions and effective docking scores were identified. The results indicated that these derivatives are good leads for dual\u2010acting COX\u20102\/5\u2010LOX inhibitors to be used as potent and safe anti\u2010inflammatory agents.<\/jats:p>","DOI":"10.1002\/ardp.201900308","type":"journal-article","created":{"date-parts":[[2020,2,7]],"date-time":"2020-02-07T11:29:22Z","timestamp":1581074962000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":23,"title":["Synthesis and biological evaluation of pyrazolone analogues as potential anti\u2010inflammatory agents targeting cyclooxygenases and 5\u2010lipoxygenase"],"prefix":"10.1002","volume":"353","author":[{"given":"Mohamed A.","family":"Shabaan","sequence":"first","affiliation":[{"name":"Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy Cairo University Cairo Egypt"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Aliaa M.","family":"Kamal","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy Cairo University Cairo Egypt"},{"name":"Department of Pharmaceutical Chemistry, Faculty of Pharmacy October University for Modern Science and Arts (MSA) Giza Egypt"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Samar I.","family":"Faggal","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy Cairo University Cairo Egypt"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Ayman E.","family":"Elsahar","sequence":"additional","affiliation":[{"name":"Department of Pharmacology and Toxicology, Faculty of Pharmacy Cairo University Cairo Egypt"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-2293-5363","authenticated-orcid":false,"given":"Khaled O.","family":"Mohamed","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy Cairo University Cairo Egypt"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"311","published-online":{"date-parts":[[2020,2,7]]},"reference":[{"key":"e_1_2_7_2_1","doi-asserted-by":"publisher","DOI":"10.1002\/med.21424"},{"key":"e_1_2_7_3_1","doi-asserted-by":"publisher","DOI":"10.1007\/978-94-015-9088-4_14"},{"key":"e_1_2_7_4_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0021-9258(18)53294-4"},{"key":"e_1_2_7_5_1","doi-asserted-by":"publisher","DOI":"10.1056\/NEJMoa050493"},{"key":"e_1_2_7_6_1","doi-asserted-by":"publisher","DOI":"10.1021\/jm0402059"},{"key":"e_1_2_7_7_1","doi-asserted-by":"publisher","DOI":"10.18433\/J3VW2F"},{"key":"e_1_2_7_8_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0165-6147(03)00077-4"},{"key":"e_1_2_7_9_1","doi-asserted-by":"publisher","DOI":"10.1136\/ard.62.6.501"},{"key":"e_1_2_7_10_1","doi-asserted-by":"publisher","DOI":"10.1371\/journal.pcbi.0030055"},{"key":"e_1_2_7_11_1","volume-title":"Inflammation and Rheumatic Diseases: The Molecular Basis of Novel Therapies","author":"Laufer S.","year":"2003"},{"key":"e_1_2_7_12_1","doi-asserted-by":"publisher","DOI":"10.1006\/phrs.2000.0784"},{"key":"e_1_2_7_13_1","doi-asserted-by":"publisher","DOI":"10.1007\/BF01966309"},{"key":"e_1_2_7_14_1","first-page":"1399","volume":"271","author":"Argentieri D. 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