Design and synthesis of 1, 3-diarylurea derivatives as selective cyclooxygenase (COX-2) inhibitors

…, S Kakhgi, A Hadipoor, B Daraee, OG Dadrass…

文献索引：Zarghi, Afshin; Kakhgi, Samaneh; Hadipoor, Atefeh; Daraee, Bahram; Dadrass, Orkideh G.; Hedayati, Mehdi Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 4 p. 1336 - 1339

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被引用次数: 14

摘要

A group of 1, 3-diarylurea derivatives, possessing a methylsulfonyl pharmacophore at the para-position of the N-1 phenyl ring, in conjunction with a N-3 substituted-phenyl ring (4-F, 4- Cl, 4-Me, 4-OMe), were designed and synthesized for evaluation as selective cyclooxygenase-2 (COX-2) inhibitors. In vitro COX-1/COX-2 isozyme inhibition structure– activity studies identified 1-(4-methylsulfonylphenyl)-3-(4-methoxyphenyl) urea (4e) as a ...