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ID: ALA1135959
Journal: Bioorg Med Chem Lett
Title: The discovery of SB-435495. A potent, orally active inhibitor of lipoprotein-associated phospholipase A(2) for evaluation in man.
Authors: Blackie JA, Bloomer JC, Brown MJ, Cheng HY, Elliott RL, Hammond B, Hickey DM, Ife RJ, Leach CA, Lewis VA, Macphee CH, Milliner KJ, Moores KE, Pinto IL, Smith SA, Stansfield IG, Stanway SJ, Taylor MA, Theobald CJ, Whittaker CM.
Abstract: The introduction of a functionalised amido substituent into a series of 1-(biphenylmethylacetamido)-pyrimidones has given a series of inhibitors of recombinant lipoprotein-associated phospholipase A(2) with sub-nanomolar potency and very encouraging developability properties. Diethylaminoethyl derivative 32, SB-435495, was selected for progression to man.
CiteXplore: 12182870