| Literature DB >> 12643913 |
Josie A Blackie1, Jackie C Bloomer, Murray J B Brown, Hung Yuan Cheng, Beverley Hammond, Deirdre M B Hickey, Robert J Ife, Colin A Leach, V Ann Lewis, Colin H Macphee, Kevin J Milliner, Kitty E Moores, Ivan L Pinto, Stephen A Smith, Ian G Stansfield, Steven J Stanway, Maxine A Taylor, Colin J Theobald.
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.Entities:
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Year: 2003 PMID： 12643913 DOI： 10.1016/s0960-894x(03)00058-1
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.940