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The discovery of SB-435495. A potent,orally active inhibitor of lipoprotein-associated phospholipase A(2) for evaluation in man |
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| 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 |
| Institution: | GlaxoSmithKline, Medicines Research Centre, Gunnels Wood Road, SG1 2NY, Stevenage, UK. |
| 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 A(2) with sub-nanomolar potency and very encouraging developability properties. Diethylaminoethyl derivative 32, SB-435495, was selected for progression to man. |
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