Synthesis and PLA(2)-inhibitory properties of 2(R)-acetamidoalkylphosphomethanols with a variable aggregate anchor

Authors
Kley, JT Von Kiedrowski, G Unger, C Massing, U
Citation
Jt. Kley et al., Synthesis and PLA(2)-inhibitory properties of 2(R)-acetamidoalkylphosphomethanols with a variable aggregate anchor, BIOORG MED, 9(2), 1999, pp. 261-264
Citations number
22
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
2
Year of publication
1999
Pages
261 - 264
Database
ISI
SICI code
0960-894X(19990118)9:2<261:SAPPO2>2.0.ZU;2-T
Abstract
Acylamino inhibitors of 14 kDa-PLA(2) were synthesized which differ in the moiety that is not bound into the enzyme's active site but immersed in the lipid aggregate when a ternary inhibitory complex is formed. Our results in dicate that this part of the inhibitors does not significantly influence in hibitory properties as long the amphiphilic character is retained. So, inhi bitory and biophysical properties should be variable independently. (C) 199 9 Elsevier Science Ltd. All rights reserved.