Synthesis and biological evaluation of indomethacin analogs possessing a N-difluoromethyl-1, 2-dihydropyrid-2-one ring system: a search for novel cyclooxygenase …

MA Chowdhury, Z Huang, KRA Abdellatif…

Index: Chowdhury, Morshed A.; Huang, Zhangjian; Abdellatif, Khaled R.A.; Dong, Ying; Yu, Gang; Velazquez, Carlos A.; Knaus, Edward E. Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 19 p. 5776 - 5780

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Citation Number: 12

Abstract

A novel class of indomethacin analogs were synthesized wherein a N-difluoromethyl-1, 2- dihydropyrid-2-one moiety (5-LOX pharmacophore) was attached at its C-4 or C-5 position via either a CO (14a–b) or CH2 (19a–b) linker to the indole N1-position. In this regard, replacement of the 4-chlorobenzoyl group present in indomethacin by N-difluoromethyl-1, 2- dihydropyrid-2-one-4-(or 5-) carbonyl and N-difluoromethyl-1, 2-dihydropyrid-2-one-4-yl ( ...