Literature DB >> 11086729

N-1 substituted pyrimidin-4-ones: novel, orally active inhibitors of lipoprotein-associated phospholipase A2.

H F Boyd1, S C Fell, S T Flynn, D M Hickey, R J Ife, C A Leach, C H Macphee, K J Milliner, K E Moores, I L Pinto, R A Porter, D A Rawlings, S A Smith, I G Stansfield, D G Tew, C J Theobald, C M Whittaker.   

Abstract

From two related series of 2-(alkylthio)-pyrimidones, a novel series of 1-((amidolinked)-alkyl)-pyrimidones has been designed as nanomolar inhibitors of human lipoprotein-associated phospholipase A2. These compounds show greatly enhanced activity in isolated plasma. Selected derivatives such as compounds 51 and 52 are orally active with a good duration of action.

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Year:  2000        PMID: 11086729     DOI: 10.1016/s0960-894x(00)00510-2

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


  5 in total

Review 1.  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 2.  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.  Myocardial infarction patients show altered lipoprotein properties and functions when compared with stable angina pectoris patients.

Authors:  Kyung-Hyun Cho; Dong-Gu Shin; Suk-Hwan Baek; Jae-Ryong Kim
Journal:  Exp Mol Med       Date:  2009-02-28       Impact factor: 8.718

4.  Females with angina pectoris have altered lipoprotein metabolism with elevated cholesteryl ester transfer protein activity and impaired high-density lipoproteins-associated antioxidant enzymes.

Authors:  Jungho Park; Jae-Ryong Kim; Dong-Gu Shin; Kyung-Hyun Cho
Journal:  Int J Mol Med       Date:  2011-12-29       Impact factor: 4.101

Review 5.  pCRP-mCRP Dissociation Mechanisms as Potential Targets for the Development of Small-Molecule Anti-Inflammatory Chemotherapeutics.

Authors:  Vittorio Caprio; Lina Badimon; Mario Di Napoli; Wen-Hui Fang; Glenn R Ferris; Baoqiang Guo; Rocco S Iemma; Donghui Liu; Yasmin Zeinolabediny; Mark Slevin
Journal:  Front Immunol       Date:  2018-05-28       Impact factor: 7.561

  5 in total

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