Novel 3-dodecanoylindole-2-carboxylic acid inhibitors of cytosolic phospholipase A(2).
Derivatives of 1-[2-(4-carboxyphenoxy)ethyl]-3-dodecanoylindole-2-carboxylic acid (4) with modified substituents at the indole-1-position were synthesized and evaluated for their ability to inhibit the arachidonic acid release in human platelets mediated by the cytosolic phospholipase A(2). One of the most active compounds obtained was 26 with an IC(50) of 0.44 microM.
Lehr
M
M
Institute of Pharmaceutical Chemistry, University of Münster, Hittorfstrasse 58-62, D-48149 Münster, Germany. lehrm@uni-muenster.de
Klimt
M
M
Elfringhoff
A S
AS
D016718:Arachidonic Acid / Q000378:metabolism; D001792:Blood Platelets / Q000187:drug effects / Q000378:metabolism; D003600:Cytosol / Q000201:enzymology; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis* / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D010741:Phospholipases A / Q000037:antagonists & inhibitors*
C438979:3-dodecanoylindole-2-carboxylic acid; D004791:Enzyme Inhibitors; D007211:Indoles; D016718:Arachidonic Acid; D010741:Phospholipases A