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Synthesis and biological evaluation of N-difluoromethyl-1, 2-dihydropyrid-2-one acetic acid regioisomers: dual inhibitors of cyclooxygenases and 5-lipoxygenase

…, MA Chowdhury, KRA Abdellatif, Y Dong, D Das…

文献索引:Yu, Gang; Praveen Rao; Chowdhury, Morshed A.; Abdellatif, Khaled R.A.; Dong, Ying; Das, Dipankar; Velazquez, Carlos A.; Suresh, Mavanur R.; Knaus, Edward E. Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 7 p. 2168 - 2173

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被引用次数: 13

摘要

A new group of acetic acid (7a–c, R1= H), and propionic acid (7d–f, R1= Me), regioisomers wherein a N-difluoromethyl-1, 2-dihydropyrid-2-one moiety is attached via its C-3, C-4, and C-5 position was synthesized. This group of compounds exhibited a more potent inhibition, and hence selectivity, for the cyclooxygenase-2 (COX-2) relative to the COX-1 isozyme. Attachment of the N-difluoromethyl-1, 2-dihydropyrid-2-one ring system to an acetic acid, ...