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ID: ALA1134222

Journal: Bioorg Med Chem Lett

Title: The identification of a potent, water soluble inhibitor of lipoprotein-associated phospholipase A2.

Authors: Boyd HF, Hammond B, Hickey DM, Ife RJ, Leach CA, Lewis VA, Macphee CH, Milliner KJ, Pinto IL, Smith SA, Stansfield IG, Theobald CJ, Whittaker CM.

Abstract: Modification of the pyrimidone 5-substituent in a series of 1-((amidolinked)-alkyl)-pyrimidones, lipophilic inhibitors of lipoprotein-associated phospholipase A2, has given inhibitors of nanomolar potency and improved physicochemical properties. Compound 23 was identified as a potent, highly water soluble. CNS penetrant inhibitor suitable for intravenous administration.

CiteXplore: 11266173

DOI: 10.1016/s0960-894x(01)00038-5