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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

DOI: 10.1016/s0960-894x(01)00678-3