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

Abstract Modification of the pyrimidone 5-substituent in a series of 1-((amidolinked)-alkyl)-pyrimidones, lipophilic inhibitors of lipoprotein-associated phospholipase A 2 , 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.