2-(Alkylthio)pyrimidin-4-ones as novel, reversible inhibitors of lipoprotein-associated phospholipase A(2)

Authors
Boyd, HF Flynn, ST Hickey, DMB Ife, RJ Jones, M Leach, CA Macphee, CH Milliner, KJ Rawlings, DA Slingsby, BP Smith, SA Stansfield, IG Tew, DG Theobald, CJ
Citation
Hf. Boyd et al., 2-(Alkylthio)pyrimidin-4-ones as novel, reversible inhibitors of lipoprotein-associated phospholipase A(2), BIOORG MED, 10(4), 2000, pp. 395-398
Citations number
9
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
4
Year of publication
2000
Pages
395 - 398
Database
ISI
SICI code
0960-894X(20000221)10:4<395:2ANRIO>2.0.ZU;2-6
Abstract
Starting from two weakly active hits from high throughput screening, a nove l series of 2-(alkylthio)-pyrimidin-4-ones with high potency and selectivit y for lipoprotein-associated phospholipase Az has been designed. In contras t to previously known inhibitors, these have been shown to act by a non-cov alent and substrate competitive mechanism. (C) 2000 Elsevier Science Ltd. A ll rights reserved.