919244-15-8Relevant articles and documents
The identification of clinical candidate SB-480848: A potent inhibitor of lipoprotein-associated phospholipase A2
Blackie, Josie A.,Bloomer, Jackie C.,Brown, Murray J. B.,Cheng, Hung-Yuan,Hammond, Beverley,Hickey, Deirdre M. B.,Ife, Robert J.,Leach, Colin A.,Lewis, V. Ann,Macphee, Colin H.,Milliner, Kevin J.,Moores, Kitty E.,Pinto, Ivan L.,Smith, Stephen A.,Stansfield, Ian G.,Stanway, Steven J.,Taylor, Maxine A.,Theobald, Colin J.
, p. 1067 - 1070 (2007/10/03)
Modification of the pyrimidone 5-substituent in clinical candidate SB-435495 has given a series of inhibitors of recombinant lipoprotein-associated phospholipase A2 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.
