The identification of a potent, water soluble inhibitor of lipoprotein-associated phospholipase A(2)

Authors
Boyd, HF Hammond, B Hickey, DMB Ife, RJ Leach, CA Lewis, VA Macphee, CH Milliner, KJ Pinto, IL Smith, SA Stansfield, IG Theobald, CJ Whittaker, CM
Citation
Hf. Boyd et al., The identification of a potent, water soluble inhibitor of lipoprotein-associated phospholipase A(2), BIOORG MED, 11(5), 2001, pp. 701-704
Citations number
8
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
5
Year of publication
2001
Pages
701 - 704
Database
ISI
SICI code
0960-894X(20010312)11:5<701:TIOAPW>2.0.ZU;2-S
Abstract
Modification of the pyrimidone 5-substituent in a series of 1-((amidolinked )-alkyl)-pyrimidones, lipophilic inhibitors of lipoprotein-associated phosp holipase A(2), has given inhibitors of nanomolar potency and improved physi cochemical properties. Compound 23 was identified as a potent, highly water soluble, CNS penetrant inhibitor suitable for intravenous administration. (C) 2001 Elsevier Science Ltd. All rights reserved.