|
|||||
|
|
2-(Alkylthio)pyrimidin-4-ones as novel, reversible inhibitors of lipoprotein-associated phospholipase A2 |
|
| Authors: | Boyd H F Flynn S T Hickey D M Ife R J Jones M Leach C A Macphee C H Milliner K J Rawlings D A Slingsby B P Smith S A Stansfield I G Tew D G Theobald C J |
| Institution: | SmithKline Beecham Pharmaceuticals, New Frontiers Science Park, Harlow, Essex, UK. |
| Abstract: | Starting from two weakly active hits from high throughput screening, a novel series of 2-(alkylthio)-pyrimidin-4-ones with high potency and selectivity for lipoprotein-associated phospholipase A2 has been designed. In contrast to previously known inhibitors, these have been shown to act by a non-covalent and substrate competitive mechanism. |
| Keywords: | |
| 本文献已被 ScienceDirect PubMed 等数据库收录！ | |