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ID: ALA1132814
Journal: Bioorg Med Chem Lett
Title: N-1 substituted pyrimidin-4-ones: novel, orally active inhibitors of lipoprotein-associated phospholipase A2.
Authors: Boyd HF, Fell SC, Flynn ST, Hickey DM, Ife RJ, Leach CA, Macphee CH, Milliner KJ, Moores KE, Pinto IL, Porter RA, Rawlings DA, Smith SA, Stansfield IG, Tew DG, Theobald CJ, Whittaker CM.
Abstract: From two related series of 2-(alkylthio)-pyrimidones, a novel series of 1-((amidolinked)-alkyl)-pyrimidones has been designed as nanomolar inhibitors of human lipoprotein-associated phospholipase A2. These compounds show greatly enhanced activity in isolated plasma. Selected derivatives such as compounds 51 and 52 are orally active with a good duration of action.
CiteXplore: 11086729