1-(Arylpiperazinylamidoalkyl)-pyrimidones: orally active inhibitors of lipoprotein-associated phospholipase A2

Jackie C. Bloomer,Helen F. Boyd,Deirdre M.B. Hickey,Robert J. Ife,Colin A. Leach,Colin H. Macphee,Kevin J. Milliner,Ivan L. Pinto,D.Anthony Rawlings,Stephen A. Smith,Ian G. Stansfield,Steven J. Stanway,Maxine A. Taylor,Colin J. Theobald,Caroline M. Whittaker

Bioorganic & Medicinal Chemistry Letters（2010）

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摘要

The lipophilic 1-substituent in a series of 1-((amidolinked)-alkyl)-pyrimidones, inhibitors of recombinant lipoprotein-associated phospholipase A2, has been modified to give inhibitors of high potency in human plasma and enhanced physicochemical properties. Phenylpiperazineacetamide derivative 23 shows very promising oral activity.

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