Immunomodulatory properties of S- and N-alkylated 5-(1H-indol-2-yl)-1, 3, 4-oxadiazole-2(3H)-thione. (February 2013)

• Record Type: Journal Article
• Authors: El Ashry, El Sayed H.; El Tamany, El Sayed H.; Abd El Fattah, Mohy El Din; Aly, Mohamed R. E.; Boraei, Ahmed T. A.; Mesaik, M. Ahmed; Abdalla, Omer M.; Fatima, Beenish; Jabeen, Almas; Shukrulla, Ahmed; Soomro, Samreen
• Is Part Of: Journal of enzyme inhibition and medicinal chemistry. Volume 28:Number 1(2013:Feb.)
• Page Start: 105
• Page End: 112
• Publication Date: 2013-02
• Subjects: Enzyme inhibitors -- Periodicals; Enzyme Inhibitors -- periodicals; Biochemistry -- periodicals; 572.7
• DOI: 10.3109/14756366.2011.636361
• Languages: English
• ISSNs: 1475-6366

Abstract

<abstract> <title> <x xml:space="preserve">Abstract</x> </title> <p>A series of <italic>S</italic>- and <italic>N</italic>-alkylated indolyloxadiazoles <bold>2–7</bold> were prepared. All compounds were tested for their immunomodulatory activity against T-cell proliferation, oxidative burst and cytokine analysis. Compounds <bold>1</bold>, <bold>2a</bold>, <bold>2b</bold>, <bold>2c</bold> and <bold>2k</bold> demonstrated highly significant (<italic>P</italic> ≤ 0.005) inhibition on PHA activated T-cell proliferation with IC₅₀ less than 3 µg/mL concentration, while <bold>3b</bold> exert a moderate inhibitory effect with IC₅₀ 8.6 µg/mL. Among all compounds of the series, only <bold>2h</bold> was found to suppress phagocytes ROS production (IC₅₀ 2.4 µg/mL) in luminol-based chemiluminescence (CL) assay. Compounds <bold>2a-k</bold> have stimulatory effect on proinflammatory cytokine predominantly IL-1β but no effect on IL-4 and NO production indicating that these compounds might have selective inhibitory effect on T-cell proliferation. Cytotoxic effect on T-cell proliferation was tested on NIH-3T3 mouse fibroblast normal cell line. All compounds were found to be free from toxic effects up to 100 μM concentration.</p> </abstract>