2. Academic Validation
  3. The discovery of SB-435495. A potent, orally active inhibitor of lipoprotein-associated phospholipase A(2) for evaluation in man

The discovery of SB-435495. A potent, orally active inhibitor of lipoprotein-associated phospholipase A(2) for evaluation in man

  • Bioorg Med Chem Lett. 2002 Sep 16;12(18):2603-6. doi: 10.1016/s0960-894x(02)00473-0.
Josie A Blackie 1,  Jackie C Bloomer,  Murray J B Brown,  Hung-Yuan Cheng,  Richard L Elliott,  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,  Caroline M Whittaker
Affiliations

Affiliation

  • 1 GlaxoSmithKline, Medicines Research Centre, Gunnels Wood Road, SG1 2NY, Stevenage, UK.
PMID: 12182870 DOI: 10.1016/s0960-894x(02)00473-0
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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