The discovery of SB-435495: A potent, orally active inhibitor of lipoprotein-Associated phospholipase A2 for evaluation in man

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.