Literature DB >> 11459662

1-(Arylpiperazinylamidoalkyl)-pyrimidones: orally active inhibitors of lipoprotein-associated phospholipase A(2).

J C Bloomer1, H F Boyd, D M Hickey, R J Ife, C A Leach, C H Macphee, K J Milliner, I L Pinto, D A Rawlings, S A Smith, I G Stansfield, S J Stanway, M A Taylor, C J Theobald, C M Whittaker.   

Abstract

The lipophilic 1-substituent in a series of 1-((amidolinked)-alkyl)-pyrimidones, inhibitors of recombinant lipoprotein-associated phospholipase A(2), 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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Year:  2001        PMID: 11459662     DOI: 10.1016/s0960-894x(01)00346-8

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  3 in total

1.  Cloning, expression, and purification of lipoprotein-associated phospholipase A(2) in Pichia pastoris.

Authors:  Fujun Zhang; Yiping Wang
Journal:  Mol Biotechnol       Date:  2006-05       Impact factor: 2.695

Review 2.  Phospholipase A2 enzymes: physical structure, biological function, disease implication, chemical inhibition, and therapeutic intervention.

Authors:  Edward A Dennis; Jian Cao; Yuan-Hao Hsu; Victoria Magrioti; George Kokotos
Journal:  Chem Rev       Date:  2011-09-12       Impact factor: 60.622

Review 3.  Lipoprotein-associated phospholipase A2: The story continues.

Authors:  Fubao Huang; Kai Wang; Jianhua Shen
Journal:  Med Res Rev       Date:  2019-05-29       Impact factor: 12.944

  3 in total

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