A new class of inhibitors of secretory phospholipase A2: enolized 1, 3-dioxane-4, 6-dione-5-carboxamides

W Breitenstein, F Märki, S Roggo, I Wiesenberg…

Index: Breitenstein, W.; Maerki, F.; Roggo, S.; Wiesenberg, I; Pfeilschifter, J.; et al. European Journal of Medicinal Chemistry, 1994 , vol. 29, # 9 p. 649 - 658

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Citation Number: 16

Abstract

Abstract Enolized 1, 3-dioxane-4, 6-dione-5-carboxamides a were identified as a new class of inhibitors of secretory phospholipase A 2 from human polymorphonuclear leucocytes (h- PMN PLA 2). Among the more than 30 compounds synthesized, the most potent inhibitors (IC 50 0.6–10 μM) were found in the series of 2, 4-disubstituted phenyl analogues of a. Compound 1a was selected for evaluation of its biological profile. This substance potently ...

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