Synthesis and biological evaluation of 2-phenylpyran-4-ones: a new class of orally active cyclooxygenase-2 inhibitors

…, A Cárdenas, L Soca, J Beleta, H Ryder…

Index: Caturla, Francisco; Jimenez, Juan-Miguel; Godessart, Nuria; Amat, Merce; Cardenas, Alvaro; Soca, Lidia; Beleta, Jordi; Ryder, Hamish; Crespo, Maria I. Journal of Medicinal Chemistry, 2004 , vol. 47, # 15 p. 3874 - 3886

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Citation Number: 24

Abstract

A series of 2-phenylpyran-4-ones were prepared and evaluated for their ability to inhibit cyclooxygenase-2 (COX-2). Extensive structure-activity relationship work was carried out within this series, and a number of potent and selective COX-2 inhibitors were identified. Compounds having a p-methylsulfone group at the 2-phenyl ring showed the best COX-2 inhibitory activity. The introduction of a substituted phenoxy ring at position 3 enhanced ...