Inhibitory effect of 4,4'-dihydroxy-α-truxillic acid derivatives on NO production in lipopolysaccharide-induced RAW 264.7 macrophages and exploration of structure-activity relationships.

Authors :: Liu SX
Jin HZ
Shan L
Zeng HW
Chen BY
Sun QY
Zhang WD
Source :: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2013 Apr 01; Vol. 23 (7), pp. 2207-11. Date of Electronic Publication: 2013 Feb 04.
Publication Year :: 2013
Abstract: The inhibitory activity of 4,4'-dihydroxy-α-truxillic acid and its derivatives (5-1a-5-35a) on nitric oxide (NO) release was evaluated in lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages. Compounds 5-3a, 5-4a, 5-5a, 5-10a, 5-24a, 5-26a and 5-30a exhibited significant inhibitory effects on NO production, with IC50 values of 19.8, 21.1, 16.4, 17.5, 20.8, 22.6 and 17.6 μM, respectively. Their cytotoxicities were also estimated using a CCK-8 assay. Among them, compound 5-10a showed no cytotoxic effect on cells up to a concentration of 50 μM. The structure-activity relationships of the compounds are also discussed.<br /> (Copyright © 2013 Elsevier Ltd. All rights reserved.)

Subjects :: Animals
Crystallography, X-Ray
Cyclobutanes chemical synthesis
Cyclobutanes chemistry
Dose-Response Relationship, Drug
Lipopolysaccharides pharmacology
Mice
Models, Molecular
Molecular Structure
Nitric Oxide biosynthesis
Structure-Activity Relationship
Cyclobutanes pharmacology
Lipopolysaccharides antagonists & inhibitors
Macrophages drug effects
Nitric Oxide antagonists & inhibitors

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