1-(Arylpiperazinylamidoalkyl)-pyrimidones: Orally active inhibitors of lipoprotein-associated phospholipase A(2)

Authors
Bloomer, JC Boyd, HF Hickey, DMB Ife, RJ Leach, CA Macphee, CH Milliner, KJ Pinto, IL Rawlings, DA Smith, SA Stansfield, IG Stanway, SJ Taylor, MA Theobald, CJ Whittaker, CM
Citation
Jc. Bloomer et al., 1-(Arylpiperazinylamidoalkyl)-pyrimidones: Orally active inhibitors of lipoprotein-associated phospholipase A(2), BIOORG MED, 11(14), 2001, pp. 1925-1929
Citations number
6
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
14
Year of publication
2001
Pages
1925 - 1929
Database
ISI
SICI code
0960-894X(20010723)11:14<1925:1OAIOL>2.0.ZU;2-L
Abstract
The lipophilic 1-substituent in a series of 1-((amidolinked)-alkyl)-pyrimid ones, inhibitors of recombinant lipoprotein-associated phospholipase A(2), has been modified to give inhibitors of high potency in human plasma and en hanced physicochemical properties. Phenylpiperazineacetamide derivative 23 shows very promising oral activity. (C) 2001 Elsevier Science Ltd. All righ ts reserved.