Phenylacetic acid regioisomers possessing a N-difluoromethyl-1, 2-dihydropyrid-2-one pharmacophore: Evaluation as dual inhibitors of cyclooxygenases and 5- …

G Yu, MA Chowdhury, KRA Abdellatif, Y Dong…

Index: Yu, Gang; Chowdhury, Morshed A.; Abdellatif, Khaled R.A.; Dong, Ying; Praveen Rao; Das, Dipankar; Velazquez, Carlos A.; Suresh, Mavanur R.; Knaus, Edward E. Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 3 p. 896 - 902

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Citation Number: 12

Abstract

A novel class of phenylacetic acid regioisomers possessing a N-difluoromethyl-1, 2- dihydropyrid-2-one pharmacophore attached to its C-2, C-3 or C-4 position was designed for evaluation as anti-inflammatory (AI) agents. A number of compounds exhibited a combination of potent in vitro cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LOX) inhibitory activities. 2-(1-Difluoromethyl-2-oxo-1, 2-dihydropyridin-4-yl) phenylacetic acid ( ...