Author/Authors :
Helen F. Boyd، نويسنده , , Sean T. Flynn، نويسنده , , Deirdre M. B. Hickey، نويسنده , , Robert J. Ife، نويسنده , , Martin Jones، نويسنده , , Colin A. Leach، نويسنده , , Colin H. Macphee، نويسنده , , Kevin J. Milliner، نويسنده , , D. Anthony Rawlings، نويسنده , , Brian P. Slingsby، نويسنده , , Stephen A. Smith، نويسنده , , Ian G. Stansfield، نويسنده , , David G. Tew، نويسنده , , Colin J. Theobald، نويسنده ,
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.