| Title : The identification of clinical candidate SB-480848: a potent inhibitor of lipoprotein-associated phospholipase A2 - Blackie_2003_Bioorg.Med.Chem.Lett_13_1067 |
| Author(s) : Blackie JA , Bloomer JC , Brown MJ , Cheng HY , 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 |
| Ref : Bioorganic & Medicinal Chemistry Lett , 13 :1067 , 2003 |
| 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. |
| ESTHER : Blackie_2003_Bioorg.Med.Chem.Lett_13_1067 |
| PubMedSearch : Blackie_2003_Bioorg.Med.Chem.Lett_13_1067 |
| PubMedID: 12643913 |
Blackie JA, Bloomer JC, Brown MJ, Cheng HY, 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 (2003)
The identification of clinical candidate SB-480848: a potent inhibitor of lipoprotein-associated phospholipase A2
Bioorganic & Medicinal Chemistry Lett
13 :1067
Blackie JA, Bloomer JC, Brown MJ, Cheng HY, 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 (2003)
Bioorganic & Medicinal Chemistry Lett
13 :1067