Details

Autor(en) / Beteiligte

• 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.

Titel

The identification of clinical candidate SB-480848: a potent inhibitor of lipoprotein-associated phospholipase A 2

Ist Teil von

• Bioorganic & medicinal chemistry letters, 2003, Vol.13 (6), p.1067-1070

Ort / Verlag

Elsevier Ltd

Erscheinungsjahr

2003

Link zum Volltext

Quelle

Alma/SFX Local Collection

Beschreibungen/Notizen

• 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. Modification of clinical candidate SB-435495 has given sub-nanomolar inhibitors of recombinant lipoprotein-associated phospholipase A 2. 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.