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ID: ALA1135094
Journal: Bioorg Med Chem Lett
Title: Potent, orally active inhibitors of lipoprotein-associated phospholipase A(2): 1-(biphenylmethylamidoalkyl)-pyrimidones.
Authors: Boyd HF, Fell SC, Hickey DM, Ife RJ, Leach CA, Macphee CH, Milliner KJ, Pinto IL, Rawlings DA, Smith SA, Stansfield IG, Stanway SJ, Theobald CJ, Whittaker CM.
Abstract: A series of 1-(biphenylmethylamidoalkyl)-pyrimidones has been designed as nanomolar inhibitors of recombinant lipoprotein-associated phospholipase A(2) with high potency in whole human plasma. 5-(Pyrazolylmethyl) derivative 16 and 5-(methoxypyrimidinylmethyl) derivative 27 demonstrated excellent pharmacodynamic profiles which correlated well with their pharmacokinetic effects.
CiteXplore: 11738571