The discovery of SB-435495: A potent, orally active inhibitor of lipoprotein-Associated phospholipase A2 for evaluation in man

Authors :: Blackie, Josie A.
Bloomer, Jackie C.
Brown, Murray J. B.
Cheng, Hung-Yuan
Elliott, Richard L.
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.
Whittaker, Caroline M.
Source :: Bioorganic & Medicinal Chemistry Letters. Sep2002, Vol. 12 Issue 18, p2603. 4p.
Publication Year :: 2002
Abstract: The introduction of a functionalised amido substituent into a series of 1-(biphenylmethylacetamido)-pyrimidones has given a series of inhibitors of recombinant lipoprotein-associated phospholipase A2 with sub-nanomolar potency and very encouraging developability properties. Diethylaminoethyl derivative 32, SB-435495, was selected for progression to man. [Copyright &y& Elsevier]

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