The identification of clinical candidate SB-480848: a potent inhibitor of lipoprotein-associated phospholipase A2

Abstract Modification of the pyrimidone 5-substituent in clinical candidate SB-435495 has given a series of inhibitors of recombinant lipoprotein-associated phospholipase A 2 with sub-nanomolar potency. Cyclopentyl fused derivative 21 , SB-480848, showed an enhanced in vitro and in vivo profile versus SB-435495 and has been selected for progression to man.